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美国赛力克生命科学HDAC信号通路,HSP信号通路,Aurora信号通路新品发布

 

靶点

HDAC (29)

Aurora Kinase (23)

HSP90 (19)

Kinesin Spindle Protein (4)

Sirtuin (3)

 

HDAC-HSP-Aurora

Aurora kinases which play a key role in cell prefabrication are serine/threonine kinases. The Aurora protein kinases family, including Aurora A, Aurora B and Aurora C, are associated to the stability of chromosome. Heat shock proteins (HSP) are a class of functionally related proteins involved in the folding and unfolding of other proteins. As molecular chaperones, Hsps bind nonnative states of other proteins and aid them to reach a functional conformation, through the expenditure of ATP. HDACs, also called Histone deacetylase appear to be core enzymes in the regulation of gene expression by binding to the negatively charged phosphate groups on the DNA backbone with its positively charged histone tails.

最新产品

PCI-34051

MPC-3100 MPC-3100是人工合成的有效的Hsp90小分子抑制剂,IC50为60 nM。

HDAC4 Antibody WB

AT13387 AT13387 是Hsp90 选择性小分子抑制剂,作用于A375, MV4-11, NCI-H1975和SKBr3细胞系时 IC50 分别为18, 12, 22和 55 nM。

Ganetespib (STA-9090) Ganetespib (STA-9090) is a unique triazolone-containing Hsp90 inhibitor with an IC50 of 4 nM for OSA 8 cells.

 

 

1 Comments

白血病治疗中的新药应用,白血病治疗激酶抑制剂列表,白血病研究新药列表

白血病治疗中的新药的应用

 

1 核苷类似物(Nucleoside analogue)

 

核苷类似物在细胞内转化成具有活性的代谢产物(三磷酸核苷类似物),而后者可抑制DNA合成。氟达拉滨(Fludarabine)与Ara-C组成的方案已经广泛用于AML的挽救性治疗并取得较好疗效。氯法拉滨(Clofarabine)是一种新的核苷酸类似物,它是一种强效的核糖核苷酸还原酶和DNA聚合酶的抑制剂。在ASH会议上有多篇有关氯法拉滨的报道,主要集中在氯法拉滨单用或分别与小剂量阿糖胞苷、或大剂量阿糖胞苷与吉姆单抗奥佐米星等组成联合方案治疗老年AML或复发难治AML11, 12, 13, 14, 15。同时还报道了新的核苷类似物如沙帕他滨(Sapacitabine)和艾西拉滨 (Elacytarabine)单独用于老年初治复发AML和难治复发AML的II期临床试验16,17。

 

Fludarabine Phosphate (Fludara) 目录号 S1229

 

Troxacitabine (Troxatyl) 目录号 S1535

 

Acyclovir (Aciclovir) 目录号 S1807

 

 

2 FLT3抑制剂(Fms-like Tyrosine kinases 3 Inhibitor)

 

AML伴FLT3-ITD表达的患者预后差,复发率高,总生存率低18。而且,这类患者若Allo-SCT移植后复发,几乎无可供选择的治疗方案。索拉非尼(Sorafanib)是一种多激酶抑制剂,通过抑制FLT3和RAF/MEK/ERK信号传导通路直接抑制肿瘤生长,已被批准用于转移性肾、肝细胞肿瘤的治疗。在本届大会上,德国Stephan19报道了他们通过问卷调查单药索拉非尼治疗复发或难治FLT3-ITD+ AML有效性及耐受性的结果。18例中5例是原发耐药者,13例是初次(11例)或再次(2例)复发。给药方法为:200-800 mg/d,中位服药时间为98天(16-425天)。所有病人均获得了HR,其中17例CR,180天的中位治疗时间后,7/18例患者出现了临床耐药。结论:单一应用索拉非尼治疗难治或复发的FLT3-ITD+ AML患者具有显著的临床疗效。索拉非尼也联合其他方案治疗FLT3-ITD+ AML,结果表明索拉非尼可减少患者的突变克隆,但是不能根除,必须同诱导及巩固治疗方案同时应用,否则疗效只是暂时性的20, 21,22 。

 

Flt 抑制剂

目录号 产品名称 产品描述 文献 客户评论

S1042 Sunitinib Malate (Sutent) Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 μM for Flk-1 and PDGFR (5) (5)

S1017 Cediranib (AZD2171) Cediranib 有效抑制VEGFR2,作用于VEGF激发的细胞增殖和KDR磷酸化时IC50分别为0.4和0.5 nM。 (2) (1)

S1119 XL-184 free base (Cabozantinib) XL-184 free base (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively.

S1490 Ponatinib (AP24534) Ponatinib是有效的可用于口服的多靶点激酶抑制剂,作用于野生型细胞,及T315I 突变细胞时IC50分别为1.2和8.8nM。

S1070 PHA-665752 PHA-665752 is c-Met inhibitor with an IC50 of 9 nM and Ki of 4 nM. (1)

S1526 AC220 (Quizartinib) AC220是有效的FLT3选择性抑制剂,IC50为2 nM。

S1101 Vatalanib dihydrochloride (PTK787) Vatalanib dihydrochloride (PTK787) is a novel VEGFR and c-Kit tyrosine kinases and angiogenesis inhibitor with IC50 of 0.037, 0.077, 0.27 and 0.73 μM for KDR, Flt-1, Flk and c-Kit, respectively. (2) (2)

S2692 TG101209 TG101209 is a potent and small molecule JAK2-selective kinase inhibitor with IC50 of 6, 25, 17 and 169 nM for JAK2, FLT3, RET and JAK3, respectively.

S2158 KW 2449 KW-2449 is a multi-kinase inhibitor of FLT3(IC50 at 6.6pM), ABL(IC50 at 14pM), ABL-T315I and Aurora kinase. (1)

S1486 AEE788 AEE788是EGFR和ErbB2的有效抑制剂,IC50分别2和6 nM。

S1470 TSU-68 (SU6668) TSU-68 (SU6668) is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 µM, 8 nM and 1.2 µM for VEGF-R1, PDGF-Rβ and FGF-R1, respectively.

S1244 MP-470 (Amuvatinib) MP-470 (Amuvatinib) is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM. (1)

S1181 ENMD-2076 ENMD-2076是有丝分裂激酶Aurora A和B选择性抑制剂,IC50分别为14 和350 nM。 (4)

S1043 Tandutinib (MLN518) Tandutinib (MLN518) is a FLT3 inhibitor. In cell-based assays tandutinib inhibited FLT3, PDGFR and KIT with IC50 values of 95-122 ng/mL.

 

3 法尼酰转移酶抑制剂(Farnesyl-transferase Inhibitor,FTI)

 

近年来研究显示Ras基因突变与髓性白血病发生有关。法尼酰基转移酶抑制剂通过抑制法尼基蛋白转移酶阻止Ras蛋白的法尼基化、裂解和羧甲基化修饰,使其失去生物活性,从而抑制了Ras信号传导通路,已成为新的很有希望的药物作用靶点。Stefania23联合法尼基转移酶抑制剂替匹法尼(Tipifarnib)和蛋白酶抑制剂硼替佐米(Bortezomib)治疗年龄大于18岁不适于传统治疗、或大于60岁复发的AML的患者。结果表明,对于高危/体弱AML患者来说,替匹法尼(±硼替佐米)可能是一个重要选择。Eric 24应用替匹法尼+/-口服依托泊苷(Etoposide)与传统的阿糖胞苷/蒽环类为主的诱导治疗进行比较,虽然缓解率不同,但他们的中位生存无明显差异(中位数6.2与7.7个月比较,p=0.82)。

 

Tipifarnib (Zarnestra) 目录号 S1453

 

 

4 组蛋白脱乙酰基酶抑制剂(Histone Deacetylase Inhibitors)

 

伏林司他(Vorinostat)是世界上第一个抑制组蛋白脱乙酰基酶的新型抗癌药物,该药于2006年获得美国FDA批准上市。伏林司他单用于治疗AML的研究已经显示出一定的疗效25。本届大会上有报道伏林司他联合伊达比星(Idarubicin, IDA)和Ara-C治疗AML和MDS中的临床II期研究,结果显示伏林司他、IDA和Ara-C联合治疗AML是安全有效的26。另外,同步或序贯联合伏林司他和地西他滨(Decitabine)治疗复发或初治的AML是有效而且没有明显的副作用,因此具有应用前景27。

 

Vorinostat (SAHA) 目录号 S1047

 

Decitabine 目录号 S1200

 

Idarubicin HCl 目录号 S1228

 

 

5 甲基化转移酶抑制剂(Methyltransferase Inhibitor)

 

地西他滨(Decitabine)是通过磷酸化后直接掺入DNA,抑制DNA甲基化转移酶,引起DNA低甲基化和细胞分化或凋亡来发挥抗肿瘤作用。本届大会有2篇关于地西他滨和GO分别应用于初治或难治/复发的AML病人的研究,结果表明地西他滨和GO的联合应用对于初治AML是有效的、毒副作用小,尤其适用于老年患者28。对于难治或复发的AML患者,以地西他滨为基础的联合治疗是一个可供选择的方案29 。本届大会还报道了甲基化转移酶抑制剂阿扎胞苷(Azacytidine)联合硼替佐米或小剂量GO治疗难治或复发AML。结果显示患者可耐受,疗效好30,31,32(表5)。

 

 

Decitabine 目录号 S1200

 

 

6.1 Voreloxin

 

Voreloxin是一类抗癌喹诺酮衍生物,通过嵌入DNA中而抑制拓扑异构酶II,从而诱导细胞凋亡。对年龄≥60岁从未接受治疗的老年AML患者来说,采用标准化疗方案并未受益,而采用Voreloxin方案,却显示了临床疗效33。

 

6.2氨萘非特(Amonafide, AS1413)

 

氨萘非特是唯一的DNA嵌入剂,II期临床试验证实氨萘非特联合Ara-C治疗老年及青年继发AML患者具有较高的缓解率和较长的缓解期34。

 

Amonafide 目录号 S1367 http://selleck.cn/amonafide-S1367.html

6.3依诺他宾(Behenoylara-C)

 

依诺他宾是在阿糖胞苷的第4位N上有三磷酰基,这样使其亲脂性提高,从而在血中(特别是血细胞中)及组织内的浓度能够维持较长时间。本品在肝、脾、肾及白血病细胞中逐渐代谢转化成阿糖胞苷,后者抑制DNA合成而显示抗肿瘤作用,是一种对急性白血病有效的抗代谢抗癌药。Taiichi35联合依诺他宾和IDA治疗初治AML165人,结果表明治疗是有效的同时也是安全的。

 

6.4来那度胺(Lenalidomide)

 

目前已有三个新药被美国FDA批准应用于治疗MDS,来那度胺是其中之一36。来那度胺治疗5q-低危MDS能达到血液学及细胞遗传学CR。在本届会议报道来那度胺治疗5q-高危MDS及5q-AML的II期临床试验,其总体缓解率达28%,部分达到细胞遗传学缓解。此结果表明来那度胺联合化疗方案治疗是可行的,且不增加额外的毒副反应37。

 

Lenalidomide (Revlimid) 目录号 S1029 http://selleck.cn/lenalidomide-S1029.html

 

 

6.5利巴韦林(Ribayirin)

 

eIF4E在人类多数恶性肿瘤(如AML)中都有过度表达,其过表达与疾病的不良预后及疾病进展有关。利巴韦林是一种抗病毒药,它的结构物理上类似mRNA7位上的G cap结构,因此可抑制eIF4E的转录。Sarit应用利巴韦林治疗AML13例,所有患者耐受性良好,无明显的副反应,有一定的临床疗效。遗憾的是所有患者对此治疗均产生耐药而复发。因此,目前正在寻找新的治疗方案同利巴韦林联合应用以克服耐药性38。

 

6.6 ARRY520

 

有丝分裂纺缍体驱动蛋白(kinesin spindle protein,KSP)对形成正常的双极纺缍体以及通过有丝分裂进行细胞增殖的细胞是必需的。ARRY520是一种高效的KSP选择抑制剂。33例AML分成单个剂量和分开剂量二组,结果显示ARRY520具有临床疗效,而且在两组中均有良好的耐受性39。

 

ARRY-520 目录号 S2737 http://selleck.cn/arry-520-S2737.html

6.7 AZD1152和AZD6244

 

Aurora B激酶是一种有丝分裂的重要调节剂,它在各种恶性肿瘤,包括AML中过表达。AZD1152是一种选择性Aurora B激酶抑制剂,能显著性抑制体内肿瘤的生长。AZD1152治疗18岁以上复发AML患者的I/II期临床试验,显示复发AML患者AZD1152的最大耐受剂量为1200mg,总的临床缓解率为23%40。AZD6244是MEK激酶抑制剂,其在初治、复发难治AML的II期临床试验中,证明是可行的41。

 

AZD1152 目录号 S1051 http://selleck.cn/azd1152-S1051.html

 

AZD1152-HQPA 目录号 S1147 http://selleck.cn/azd1152-hqpa-S1147.html

 

AZD6244 (Selumetinib) 目录号 S1008 http://selleck.cn/azd6244-selumetinib-S1008.html

 

 

6.8 Terameprocol

 

凋亡蛋白抑制剂存活素在细胞增殖及细胞周期调节网络中发挥着重要的作用。存活素能维持白血病细胞的存活,使白血病细胞对化疗及FLT-3抑制剂治疗耐药。实验表明,针对存活素的靶向治疗能抑制白血病细胞的活性。在本届大会报告一项临床试验,用存活素和cdc2 (CDK1)的抑制剂Terameprocol (EM-1421)治疗进展性血液恶性肿瘤。16例分为3组,分别给予不同剂量的Terameproco治疗,患者平均接受了2个周期的治疗。研究证明该药是安全的,且具有临床疗效42。

 

总结与展望

AML的治疗正在进入一个崭新的时代,我们依据本届年会对AML的诱导缓解治疗、难治或复发治疗的最新方案以及新药的临床应用,尤其是新的核苷类似物、多种酶的抑制剂等作一介绍。总之,随着对AML研究的不断深入,治疗方案的不断完善,各种新型细胞毒药物、分子靶向药物及单克隆抗体的不断涌现,我们有理由相信AML患者的生存率将有明显提高。

 

 

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抑制剂分子库列表,美国Selleck高特异性分子库/高通量筛选列表,赛导通生物科技现货供应

 

首页 >> 分子库/高通量筛选 >> 抑制剂分子库

 

 

抑制剂分子库 (96孔板)产品目录号. L1100

粉末:

剂量 价格

1mg/well ¥ 112833

2mg/well ¥ 186543

预溶在DMSO中:

剂量 价格

100μL/well (10mM solution) ¥ 75033

250μL/well (10mM solution) ¥ 114723

Customize Your Library

联系我们

描述&优势

326种药物抑制剂的独特集合,可用于高通量筛选和高内涵筛选 。

通过前期临床研究和临床实验,生物活性和安全性得到验证。

其中一些抑制剂已经得到FDA批准

作用于PI3K, VEGFR和RTK通路,HDAC, Aurora激酶, CDK和细胞周期调节,整合酶/蛋白酶,等等。

结构多样,药效显著,可渗透细胞。

具有充分详细的结构说明,IC50值,及客户反馈资料。

NMR和HPLC技术保证产品高纯度。

产品详细信息

配制: 326种抑制剂制成冻干粉或预溶在DMSO溶液中

96-孔板: 是

储存: -80°C 长期储存

稳定性: 6个月

发货: 蓝冰物流

包装: 惰性气体

抑制剂分子库目录册

下载抑制剂分子库目录册 - SDF格式下载抑制剂分子库目录册 - XLSX格式

抑制剂分子库全部组成

 

 

下载产品目录册及宣传资料

 

使用我公司Selleck产品的论文

The Anandamide Effect on NO/cGMP Pathway in Human Platelets

[Maria Grazia Signorello,Enrica Giacobbe et al. Journal of Cellular Biochemistry. 2011;112:924-932]

Synergy between inhibitors of androgen receptor and MEK has therapeutic implications in estrogen receptor-negative breast cancer

[Ali Naderi, Kee Ming Chia et al. Breast Cancer Research. 2011;13:762-770]

Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF

[Jiancheng Hu, Haiyang Yu et al. PNAS. 2011 April;108:6067-6072]

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

[Ramin Nazarian,Hubing Shi et al. nature. 2010 December;468:973-979]

Targeting Mitotic Exit Leads to Tumor Regression In Vivo: Modulation by Cdk1, Mastl,and the PP2A/B55α,β Phosphatase

[Eusebio Manchado,María Guillamot et al. Cancer Cell. 2010 December;18:641-654]

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

[V Serra, M Scaltriti et al. Oncogene. 2011;1]

Embryonic lethal phenotype reveals a function of TDG in maintaining epigenetic stability

[Daniel Corta´zar,Christophe Kunz et al. Nature. 2011 February;470:419-423]

Identification and Characterization of Persistent Intracellular Human Immunodeficiency Virus Type 1 Integrase Strand Transfer Inhibitor Activity

[Yasuhiro Koh, Hillel Haim et al. Antimicrobial agents and chemotherapy. 2011 Jan;55:42-49]

Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro

[Nadine Ce´cile Luise Zembruski,Gabriele Bu¨chel et al. Journal Antimicrob Chemother. 2011 January;11]

查看其它分子库

L1200

激酶抑制剂分子库

提供141种激酶抑制剂的集合

L1800

酪氨酸激酶抑制剂分子库

提供86种酪氨酸激酶抑制剂集合

L1300

FDA批准的原料药库

提供381种FDA批准的原料药集合

L1400

天然产物库

130种天然产物的集合

L1500

化疗药物库

40种化疗药物的集合

L1700

化合物库

提供703种具有生物活性化合物的集合

 

 

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化合物库列表,美国Selleck高特异性分子库/高通量筛选列表,赛导通生物科技现货供应

首页 >> 分子库/高通量筛选 >> 化合物库

 

 

化合物库 (96孔板)产品目录号. L1700

粉末:

剂量 价格

1mg/well ¥ 171423

2mg/well ¥ 254583

预溶在DMSO中:

剂量 价格

100μL/well (10mM solution) ¥ 107163

250μL/well (10mM solution) ¥ 173313

Customize Your Library

联系我们

描述&优势

703种具有生物活性的化合物的独特集合,可用于高通量筛选和高内涵筛选 。

通过前期临床研究和临床实验,生物活性和安全性得到验证。

其中一些化合物已经得到FDA批准 。

包括大部分Selleck 抑制剂,原料药,天然产物,和化疗药物等。

结构多样,药效显著,可渗透细胞。

具有充分详细的结构说明,IC50值,及客户反馈资料。

NMR和HPLC技术保证产品高纯度。

产品详细信息

配制: 703种具有生物活性的化合物制成冻干粉或预溶在DMSO溶液中。

96-孔板: 是

储存: -80°C 长期储存

稳定性: 6个月

发货: 蓝冰物流

包装: 惰性气体

化合物库目录册

下载化合物库目录册 - SDF格式下载化合物库目录册 - XLSX格式

化合物库全部组成

 

 

下载产品目录册及宣传资料

 

使用我公司Selleck产品的论文

Targeting Mitotic Exit Leads to Tumor Regression In Vivo: Modulation by Cdk1, Mastl,and the PP2A/B55α,β Phosphatase

[Eusebio Manchado,María Guillamot et al. Cancer Cell. 2010 December;18:641-654]

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

[V Serra, M Scaltriti et al. Oncogene. 2011;1]

Embryonic lethal phenotype reveals a function of TDG in maintaining epigenetic stability

[Daniel Corta´zar,Christophe Kunz et al. Nature. 2011 February;470:419-423]

Identification and Characterization of Persistent Intracellular Human Immunodeficiency Virus Type 1 Integrase Strand Transfer Inhibitor Activity

[Yasuhiro Koh, Hillel Haim et al. Antimicrobial agents and chemotherapy. 2011 Jan;55:42-49]

Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro

[Nadine Ce´cile Luise Zembruski,Gabriele Bu¨chel et al. Journal Antimicrob Chemother. 2011 January;11]

The Anandamide Effect on NO/cGMP Pathway in Human Platelets

[Maria Grazia Signorello,Enrica Giacobbe et al. Journal of Cellular Biochemistry. 2011;112:924-932]

Synergy between inhibitors of androgen receptor and MEK has therapeutic implications in estrogen receptor-negative breast cancer

[Ali Naderi, Kee Ming Chia et al. Breast Cancer Research. 2011;13:762-770]

Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF

[Jiancheng Hu, Haiyang Yu et al. PNAS. 2011 April;108:6067-6072]

 

0 Comments

激酶抑制剂分子库列表,美国Selleck高特异性分子库/高通量筛选列表,赛导通生物科技现货供应

 

首页 >> 分子库/高通量筛选 >> 激酶抑制剂分子库

 

 

激酶抑制剂分子库 (96孔板)产品目录号. L1200

粉末:

剂量 价格

1mg/well ¥ 63693

2mg/well ¥ 103950

预溶在DMSO中:

剂量 价格

100μL/well (10mM solution) ¥ 41013

250μL/well (10mM solution) ¥ 64260

Customize Your Library

联系我们

描述&优势

141种激酶抑制剂的独特集合,可用于高通量筛选和高内涵筛选 。

通过前期临床研究和临床实验,生物活性和安全性得到验证。

其中一些激酶抑制剂已得到FDA批准 。

作用于激酶,如RTKs, PI3K, Aurora激酶, CDK和MEK。

大部分为ATP竞争性抑制剂。

结构多样,药效显著,可渗透细胞。

具有充分详细的结构说明,IC50值,及客户反馈资料。

NMR和HPLC技术保证产品高纯度。

产品详细信息

配制: 141种激酶种抑制剂制成冻干粉或预溶在DMSO溶液中。

96-孔板: 是

储存: -80°C 长期储存

稳定性: 6个月

发货: 蓝冰物流

包装: 惰性气体

激酶抑制剂分子库目录册

下载激酶抑制剂分子库目录册 - SDF格式下载激酶抑制剂分子库目录册 - XLSX格式

激酶抑制剂分子库全部组成

 

 

下载产品目录册及宣传资料

 

使用我公司Selleck产品的论文

Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuroblastoma Tumor-Initiating Cells

[Natalie Grinshtein, Alessandro Datti et al. Cancer Res. 2011 February;71:1385-1395]

A Feedback Loop between Androgen Receptor and ERK Signaling in Estrogen Receptor–Negative Breast Cancer

[Kee Ming Chia,Ji Liu et al. Neoplasia. 2011;13:154-166]

Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors

[Christine M Lovly, Johannes M Heuckmann et al. Cancer Res. 2011 May]

Tyrosine kinase inhibitors for the treatment of acute myeloid leukemia: Delineation of anti-leukemic mechanisms of action

[Elodie Lainey, Sylvain The´pot et al. Biochemical Pharmacology. 2011;1]

Targeting zebrafish and murine pituitary corticotroph tumors with a cyclin-dependent kinase (CDK) inhibitor

[Ning-Ai Liu, Hong Jiang et al. PNAS. 2011 May;108:8414-8419]

Evasion Mechanisms to Igf1r Inhibition in Rhabdomyosarcoma

[Jinu Abraham, Suresh I. Prajapati et al. Mol Cancer Ther. 2011 April;10:697-707]

Platelet-derived Growth Factor Receptor Alpha Overexpression Cooperates With INK4A/ARF Loss to Promote Gliomagenesis—Roles of SHP-2 and PI3K Pathways

[Masanobu Takahashi,Minoru Koi et al. Journal of biological chemistry. 2011 April;286:12157-12165]

Peroxiredoxin II Restrains DNA Damage-induced Death in Cancer Cells by Positively Regulating JNK-dependent DNA Repair

[Kyung Wha Lee,Doo Jae Lee et al. Journal of biological chemistry. 2011 March;286:8394-8404]

Dasatinib Plus Nutlin-3 Shows Synergistic Antileukemic Activity in Both p53wild-type and p53mutated B Chronic Lymphocytic Leukemias by Inhibiting the Akt Pathway

[Giorgio Zauli, Rebecca Voltan et al. Clin Cancer Res. 2011;17:762-770]

查看其它分子库

L1100

抑制剂分子库

提供326种最新药物抑制剂的集合

L1800

酪氨酸激酶抑制剂分子库

提供86种酪氨酸激酶抑制剂集合

L1300

FDA批准的原料药库

提供381种FDA批准的原料药集合

L1400

天然产物库

130种天然产物的集合

L1500

化疗药物库

40种化疗药物的集合

L1700

化合物库

提供703种具有生物活性化合物的集合

 

 

0 Comments

酪氨酸激酶抑制剂分子库列表,美国Selleck高特异性分子库/高通量筛选列表,赛导通生物科技现货供应

 

首页 >> 分子库/高通量筛选 >> 酪氨酸激酶抑制剂分子库

 

 

酪氨酸激酶抑制剂分子库 (96孔板)产品目录号. L1800

粉末:

剂量 价格

1mg/well ¥ 41580

2mg/well ¥ 67473

预溶在DMSO中:

剂量 价格

100μL/well (10mM solution) ¥ 27783

250μL/well (10mM solution) ¥ 42903

Customize Your Library

Contact Us

描述&优势

86种酪氨酸激酶抑制剂的独特集合,可用于高通量筛选和高内涵筛选 。

通过前期临床研究和临床实验,生物活性和安全性得到验证。

其中一些抑制剂已经得到FDA批准。

作用于酪氨酸激酶,如EGFR,VEGFR,SRC,c-Met,和JAK 。

结构多样,药效显著,可渗透细胞。

具有充分详细的结构说明,IC50值,及客户反馈资料。

NMR和HPLC技术保证产品高纯度。

产品详细信息

配制: 86种酪氨酸激酶抑制剂制成冻干粉或预溶在DMSO溶液中。

96-孔板: 是

储存: -80°C 长期储存

稳定性: 6个月

发货: 蓝冰物流

包装: 惰性气体

酪氨酸激酶抑制剂分子库目录册

下载酪氨酸激酶抑制剂分子库目录册 - SDF格式下载酪氨酸激酶抑制剂分子库目录册 - XLSX格式

酪氨酸激酶抑制剂分子库全部组成

 

 

下载产品目录册及宣传资料

 

使用我公司Selleck产品的论文

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

[Ramin Nazarian,Hubing Shi et al. nature. 2010 December;468:973-979]

Targeting Mitotic Exit Leads to Tumor Regression In Vivo: Modulation by Cdk1, Mastl,and the PP2A/B55α,β Phosphatase

[Eusebio Manchado,María Guillamot et al. Cancer Cell. 2010 December;18:641-654]

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

[V Serra, M Scaltriti et al. Oncogene. 2011;1]

Embryonic lethal phenotype reveals a function of TDG in maintaining epigenetic stability

[Daniel Corta´zar,Christophe Kunz et al. Nature. 2011 February;470:419-423]

Identification and Characterization of Persistent Intracellular Human Immunodeficiency Virus Type 1 Integrase Strand Transfer Inhibitor Activity

[Yasuhiro Koh, Hillel Haim et al. Antimicrobial agents and chemotherapy. 2011 Jan;55:42-49]

Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro

[Nadine Ce´cile Luise Zembruski,Gabriele Bu¨chel et al. Journal Antimicrob Chemother. 2011 January;11]

The Anandamide Effect on NO/cGMP Pathway in Human Platelets

[Maria Grazia Signorello,Enrica Giacobbe et al. Journal of Cellular Biochemistry. 2011;112:924-932]

Synergy between inhibitors of androgen receptor and MEK has therapeutic implications in estrogen receptor-negative breast cancer

[Ali Naderi, Kee Ming Chia et al. Breast Cancer Research. 2011;13:762-770]

Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF

 

0 Comments

FDA批准的原料药库列表,美国Selleck高特异性分子库/高通量筛选列表,赛导通生物科技现货供应

首页 >> 分子库/高通量筛选 >> FDA批准的原料药库

 

 

FDA批准的原料药库 (96孔板)产品目录号. L1300

粉末:

剂量 价格

1mg/well ¥ 42903

2mg/well ¥ 58023

预溶在DMSO中:

剂量 价格

100μL/well (10mM solution) ¥ 22113

250μL/well (10mM solution) ¥ 44793

Customize Your Library

Contact Us

描述&优势

381种FDA批准的原料药的独特集合,可用于高通量筛选和高内涵筛选 。

帮助已有药物定位新的靶点。

通过临床实验,生物活性和安全性得到验证。

全部得到FDA批准。

与肿瘤学,心脏病理学, 抗炎反应,免疫学,神经医学, 痛觉缺失等等都有关。

结构多样,药效显著,可渗透细胞。

具有充分详细的结构说明,IC50值,及客户反馈资料。

NMR和HPLC技术保证产品高纯度。

产品详细信息

配制: 381种FDA批准的原料药制成冻干粉或预溶在DMSO溶液中。

96-孔板: 是

储存: -80°C 长期储存

稳定性: 6个月

发货: 蓝冰物流

包装: 惰性气体

FDA批准的原料药库目录册

如果您需要下载FDA批准的原料药库目录册(.xlxs和.SDF),请通过 info@selleckchem.com联系我们

FDA批准的原料药库全部组成

 

 

下载产品目录册及宣传资料

 

使用我公司Selleck产品的论文

Anti-myeloma activity of a multi targeted kinase inhibitor,AT9283, via potent Aurora Kinase and STAT3 inhibition either alone or in combination with lenalidomide.

[Loredana Santo, Teru Hideshima et al. Clin Cancer Res. 2011 May;17:3259-3271]

Dasatinib Plus Nutlin-3 Shows Synergistic Antileukemic Activity in Both p53wild-type and p53mutated B Chronic Lymphocytic Leukemias by Inhibiting the Akt Pathway

[Giorgio Zauli, Rebecca Voltan et al. Clin Cancer Res. 2011;17:762-770]

Rotavirus Replication Requires a Functional Proteasome for Effective Assembly of Viroplasms

[R. Contin,F. Arnoldi et al. Journal of virology. 2011 Mar;85:2781-2792]

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

[V Serra, M Scaltriti et al. Oncogene. 2011;1]

Identification and Characterization of Persistent Intracellular Human Immunodeficiency Virus Type 1 Integrase Strand Transfer Inhibitor Activity

[Yasuhiro Koh, Hillel Haim et al. Antimicrobial agents and chemotherapy. 2011 Jan;55:42-49]

Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro

[Nadine Ce´cile Luise Zembruski,Gabriele Bu¨chel et al. Journal Antimicrob Chemother. 2011 January;11]

Tyrosine kinase inhibitors for the treatment of acute myeloid leukemia: Delineation of anti-leukemic mechanisms of action

[Elodie Lainey, Sylvain The´pot et al. Biochemical Pharmacology. 2011;1]

Sorafenib induces apoptotic cell death in human non-small cell lung cancer cells by down-regulating mammalian target of rapamycin (mTOR)-dependent survivin expression

[Young-Sun Kim, Hyeon-Ok Jin et al. Biochemical Pharmacology. 2011 August;82:216-226 ]

 

0 Comments

天然产物库列表,美国Selleck高特异性分子库/高通量筛选列表,赛导通生物科技现货供应

首页 >> 分子库/高通量筛选 >> 天然产物库

 

 

天然产物库 (96孔板)产品目录号. L1400

粉末:

剂量 价格

1mg/well ¥ 26460

2mg/well ¥ 39123

预溶在DMSO中:

剂量 价格

100μL/well (10mM solution) ¥ 17331

250μL/well (10mM solution) ¥ 27783

Customize Your Library

联系我们

描述&优势

130种天然产物的独特集合,可用于高通量筛选和高内涵筛选 。

结构多样,药效显著,可渗透细胞。

具有充分详细的结构说明,IC50值,及客户反馈资料。

NMR和HPLC技术保证产品高纯度。

产品详细信息

配制: 130种天然产物制成冻干粉或预溶在DMSO溶液中。

96-孔板: 是

储存: -80°C 长期储存

稳定性: 6个月

发货: 蓝冰物流

包装: 惰性气体

天然产物库目录册

下载天然产物库目录册 - SDF格式下载天然产物库目录册 - XLSX格式

产看其它分子库

L1100

抑制剂分子库

提供326种最新药物抑制剂的集合

L1200

激酶抑制剂分子库

提供141种激酶抑制剂的集合

L1800

酪氨酸激酶抑制剂分子库

提供86种酪氨酸激酶抑制剂集合

L1300

FDA批准的原料药库

提供381种FDA批准的原料药集合

L1500

化疗药物库

40种化疗药物的集合

L1700

化合物库

提供703种具有生物活性化合物的集合

 

 

 

0 Comments

化疗药物库列表,美国Selleck高特异性分子库/高通量筛选列表,赛导通生物科技现货供应

 

 

首页 >> 分子库/高通量筛选 >> 化疗药物库

 

 

化疗药物库 (96孔板)产品目录号. L1500

粉末:

剂量 价格

1mg/well ¥ 8883

2mg/well ¥ 14553

预溶在DMSO中:

剂量 价格

100μL/well (10mM solution) ¥ 5670

250μL/well (10mM solution) ¥ 9450

Customize Your Library

联系我们

描述&优势

40种化疗药物的独特集合,可用于高通量筛选和高内涵筛选 。

通过临床实验,生物活性和安全性得到验证。

其中一些化疗药物已经得到FDA批准,用于肿瘤和非肿瘤治疗。

结构多样,药效显著,可渗透细胞。

具有充分详细的结构说明,IC50值,及客户反馈资料。

NMR和HPLC技术保证产品高纯度。

产品详细信息

配制: 40种化疗药物制成冻干粉或预溶在DMSO溶液中。

96-孔板: 是

储存: -80°C 长期储存

稳定性: 6个月

发货: 蓝冰物流

包装: 惰性气体

化疗药物库目录册

如果您需要下载化疗药物库目录册(.xlxs和.SDF),请通过 info@selleckchem.com联系我们

化疗药物库全部组成

 

 

下载产品目录册及宣传资料

 

使用我公司Selleck产品的论文

Sorafenib induces apoptotic cell death in human non-small cell lung cancer cells by down-regulating mammalian target of rapamycin (mTOR)-dependent survivin expression

[Young-Sun Kim, Hyeon-Ok Jin et al. Biochemical Pharmacology. 2011 August;82:216-226 ]

Anti-myeloma activity of a multi targeted kinase inhibitor,AT9283, via potent Aurora Kinase and STAT3 inhibition either alone or in combination with lenalidomide.

[Loredana Santo, Teru Hideshima et al. Clin Cancer Res. 2011 May;17:3259-3271]

Molecular Characterization of c-Abl/c-Src Kinase Inhibitors Targeted against Murine Tumour Progenitor Cells that Express Stem Cell Markers

[Thomas Kruewel, Silvia Schenone et al. PLoS One. 2010 November;5]

Global lymphoid tissue remodeling during a viral infection is orchestrated by a B celllymphotoxin-dependent pathway

[Varsha Kumar, Elke Scandella et al. BLOOD. 2010 June;115:4725-4733]

Sunitinib deregulates tumor adaptation to hypoxia by inhibiting HIF-1α synthesis in HT-29 colon cancer cells

Hyun-Woo Shin, Chung-Hyun Cho et al. Biochemical and Biophysical Research Communications. 2010;398:205-211

查看其它分子库

L1100

抑制剂分子库

提供326种最新药物抑制剂的集合

L1200

激酶抑制剂分子库

提供141种激酶抑制剂的集合

L1800

酪氨酸激酶抑制剂分子库

提供86种酪氨酸激酶抑制剂集合

L1300

FDA批准的原料药库

提供381种FDA批准的原料药集合

L1400

天然产物库

130种天然产物的集合

L1700

化合物库

提供703种具有生物活性化合物的集合

客户反馈数据

 

Data independently produced by Dr Helen Sadik of Johns Hopkins University

Capecitabine (Xeloda) purchased from Selleck

Cells were seeded in 96 well paltes, and then treated with the indicated concentration of Capecitabine for 48h. Cell survival was measured by a standarad MTT assay.

 

 

 

Data independently produced by Dr Helen Sadik of Johns Hopkins University

Carboplatin purchased from Selleck

A. MCF10A-Ras overexpressing a vector control or the gene of interest (GeneX), or MCF7 expressing a scramble or a siRNA for the geneX were treated with DMSO or with Carboplatin for 24h. Resistant colonies were allowed to grow for 2 weeks, and are then stained with Crystal Violet. B. Quantification of the results.

 

Data independently produced by Dr Helen Rizos from the university of Sydney

Imatinib Mesylate purchased from Selleck

A. Viability curve for the c-Kit mutant MelMS melanoma cell line treated with increasing concentrations of imatinib for 72h (relative to DMSO-treated controls; mean ± sd; n=3) B. MelMS melanoma cells were treated with 50nM imatinib for 24h. The effects on c-Kit, ERK and AKT activation were determined by immunoblotting.

 

Data independently produced by Dr Helen Sadik of Johns Hopkins University

Gemcitabine Hydrochloride (Gemzar) purchased from Selleck

Cells were seeded in 96 well paltes, and then treated with the indicated concentration of Gemcitabine for 48h. Cell survival was measured by a standarad MTT assay.

 

 

 

Data from [Cancer Cell 2011.June;19:1–13]

Rapamycin (Sirolimus) purchased from Selleck

Cooperative Effects of AR and mTOR Inhibition In Vitro and In Vivo (A) In vitro response of Pten null;Ar+ murine (CaP8) and human (LNCaP) prostate cancer cells to AR knockdown (sh-AR) or pharmacological inhibition of AR (MDV3100, 10 mM) with and without rapamycin (R: 1 nM) treatment (Sc, control sh oligo). (B and D) In vivo response to treatments with castration, MDV3100, rapamycin, or their combinations as measured by cell proliferation (Ki67+cells) and (C and D) tumor burden in Pb-Cre+;-PtenL/L and Pb-Cre+;PtenL/L:ArL/Y mutants. Scale bars represent 2 mm (C), 200 mm (D), and 75 mm (D, inset). Error bars represent mean ± SD.

 

Data from [Biochem Bioph Res Co 2010 June;398:205–211]

Sunitinib Malate (Sutent) purchased from Selleck

Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 lm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 lm diameter) dis

 

 

0 Comments

现货,BI6727 (Volasertib),CAS号:755038-65-4,美国进口,细胞周期(Cell Cycle / Checkpoint), PLK , PLK 抑制剂,selleck,S2235

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> PLK >> PLK 抑制剂 >> BI6727 (Volasertib)http://www.selleck.cn/bi6727-volasertib-S2235.html

技术数据:

分子量(MW): 618.81

化学式:

C34H50N8O3

 

溶解度: DMSO ≥23mg/mL Water <1mg/mL Ethanol ≥124mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 755038-65-4

生物活性

 

 

BI 6727 is a highly potent Polo-like kinase inhibitor with an IC50 of 0 .87 nM BI 6727 has an EC50 of 11-37 nM on a panel of cancer cell lines and selective dihydropteridinone with distinct properties. BI 6727 has a pharmacokinetic profile favoring sustained exposure of tumor tissues with a high volume of distribution and a long terminal half-life in mice. BI 6727 has physicochemical and pharmacokinetic properties that allow in vivo testing of i.v. as well as oral formulations, adding flexibility to dosing schedules. BI 6727 shows marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer. [1][2][3]

 

 

 

参考文献

BI 6727, A Polo-like Kinase Inhibitor with Improved Pharmacokinetic Profile and Broad Antitumor Activity Martin Steegmaier, Matthias Hoffmann, et al. Clin Cancer Res 2009;15:3094-3102

Polo-Like Kinase (PLK) Inhibitors in Preclinical and Early Clinical Development in Oncology PATRICK SCHÖFFSKI The Oncologist 2009;14:559–570

Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuroblastoma Tumor-Initiating Cells Alessandro Datti, Mayumi Fujitani, et al. Cancer Res 2011;71:1385-1395

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3、因您个人原因造成的商品损坏(如自行使用、分装、受潮、变质、非原物品的等)将不予退换。

4、Selleck目前只支持商品一换一服务,换货时无法加定商品。

5、如您购买商品时Selleck上海办事处已向您提供发票,则办理退货或订单金额发生变更的换货时,请将发票随商品一同返还给Selleck上海办事处赛导通生物科技(上海)有限公司,请您妥善保管发票,如发票丢失,将无法办理退换货。

6、您的订单若办理退换货,运费金额会在您的实际退款中扣除。

 

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现货,LDE225 (NVP-LDE225) ,CAS号:956697-53-3,美国进口,G蛋白偶联受体(GPCR & G P) ,Smoothened , Smoothened 抑制剂,selleck,S2151

信号转导通路: G蛋白偶联受体(GPCR & G P) >> Smoothened >> Smoothened 抑制剂 >> LDE225 (NVP-LDE225)http://www.selleck.cn/lde225-nvp-lde225-S2151.html

技术数据:

分子量(MW): 485.5

化学式:

C26H26F3N3O3

 

溶解度: DMSO ≥97mg/mL Water <1mg/mL Ethanol ≥97mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 956697-53-3

生物活性

 

 

LDE225 (NVP-LDE225) is a novel and specific, orally bioavailable Smo inhibitor with an IC50 of 11 nM. It has been shown to potentially inhibit Hh-and Smo-dependent proliferation in vivo. It also induced the regression of preformed basaloid lesions with an IC50 of <150 nmol/l and almost complete regression at 1.5 μmol/l. Topical application of a 1% LDE225 (NVP-LDE225) solution to depilated skin of C57/BL6 mice completely inhibited hair growth during anagen phase as well as the expression of the Hh-pathway target genes (Gli1, Gli2, Sox9, and N-Myc) and partial inhibition was obtained when applying a 0.3% solution. [1][2]

 

 

 

参考文献

Melanoma Research 2010;20:e40

Melanoma Research 2010;20:e70

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现货,Zibotentan (ZD4054),CAS号:186497-07-4,美国进口,G蛋白偶联受体(GPCR & G P) ,ETA-receptor,ETA-receptor 抑制剂和化合物,selleck,S1456

信号转导通路: G蛋白偶联受体(GPCR & G P) >> ETA-receptor >> ETA-receptor 抑制剂 >> Zibotentan (ZD4054)http://www.selleck.cn/zibotentan-zd4054-S1456.html

技术数据:

分子量(MW): 424.43

化学式:

C19H16N6O4S

 

溶解度: DMSO ≥14mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 186497-07-4

生物活性

 

 

Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). It was first evaluated as a potential treatment for pulmonary arterial hypertension in the late 1990s. Subsequently, interest switched to the role of endothelins in cancer, particularly hormone-resistant prostate cancer (HRPC).

In vitro, Zibotentan (ZD4054) has been shown to compete with 125I-ET-1 for binding to the cloned human ETA-receptor with an IC50 value of 21 nM. No binding to the ETB receptor was observed with concentrations of zibotentan in excess of 10 μM.

This agent is capable of inhibiting or reducing the multitude of effects that are evoked by ET-1 activation of the ETA receptor and which promote tumor survival, growth and progression. Zibotentan (ZD4054)treatment produced significant inhibition of tumor growth in ovarian and breast xenografts.[1]

 

 

 

参考文献

The disposition and metabolism of zibotentan (ZD4054): an oral-specific endothelin A receptor antagonist in mice, rats and dogs. Clarkson-Jones JA et al. Xenobiotica. 2011 Sep;41(9):784-96.

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现货,SB 202190 ,CAS号:152121-30-7,美国进口,MAPK , p38 MAPK , p38 MAPK 抑制剂和化合物,,selleck,S1077

信号转导通路: MAPK >> p38 MAPK >> p38 MAPK 抑制剂和化合物 >> SB 202190http://selleck.cn/sb-202190-S1077.html

技术数据:

分子量(MW): 331.34

化学式:

C20H14N3OF

 

溶解度: DMSO ≥66mg/mL Water <1mg/mL Ethanol ≥32mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 152121-30-7

生物活性

 

 

SB202190 enhanced the growth of THP-1 and MV4-11 cells. In the presence of SB202190, the ED50 values for the farnesyltransferase inhibitor FPT inhibitor II and MEK inhibitor U0126 were significantly decreased.SB202190 increased the phosphorylation of C-Raf and extracellular regulated kinase (ERK). [1]

SB202190 suppressed the kinase activity of p38, leading to inhibition of activation of MAPKAPK2 and then the subsequent phosphorylation of hsp27 in LPS-treated macrophages both in vitro and in vivo. [2]

SB202190 blocked p38 half maximally at 30 nM. Concentrations as high as 30,000 nM did not inhibit ERK and JNK activity. [3]

 

 

 

参考文献

Activation of the ras genes in malignant and premalignant colorectal tumors. Glarakis IS, et al. Oncol Rep. 1998 Nov-Dec;5(6):1451-4.

Transformation of mammalian cells by constitutively active MAP kinase kinase Mansour SJ,et al. Science 1994;265(5174):966-970

p38 MAP kinase inhibition promotes primary tumour growth via VEGF independent mechanism. O'Sullivan AW,et al. World J Surg Oncol. 2009 Nov 15;7:89.

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0 Comments

现货,PHT-427 , CAS1191951-57-1,美国进口,PI3K / mTOR / AKT, AKT , AKT 抑制剂和化合物,selleck,S1556

信号转导通路: PI3K / mTOR / AKT >> AKT >> AKT 抑制剂和化合物 >> PHT-427http://selleck.cn/pht-427-S1556.html

技术数据:

分子量(MW): 409.61

化学式:

C20H31N3O2S2

 

溶解度: DMSO ≥82mg/mL Water ≥5mg/mL Ethanol ≥82mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1191951-57-1

生物活性

 

 

PHT-427 is a Novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. It inhibited Akt and PDPK1 signaling and their downstream targets in sensitive but not resistant cells and tumor xenografts. When given orally, PHT-427 inhibited the growth of human tumor xenografts in immunodeficient mice, with up to 80% inhibition in the most sensitive tumors, and showed greater activity than analogues with C4, C6, or C8 alkyl chains. Inhibition of PDPK1 was more closely correlated to antitumor activity than Akt inhibition. [1]

 

 

 

参考文献

Molecular pharmacology and antitumor activity of PHT-427 a novel AKT/PDPK1 pleckstrin homology domain inhibitor Emmanuelle J. Meuillet,Song Zuohe,et al. Mol Cancer Ther 2010 March;9(3): 706–717

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现货,SB590885,CAS号:405554-55-4,美国进口,MAPK, Raf , Raf 抑制剂和化合物,selleck,S2220

信号转导通路: MAPK >> Raf >> Raf 抑制剂 >> SB590885http://www.selleck.cn/sb590885-S2220.html

技术数据:

分子量(MW): 453.54

化学式:

C27H27N5O2

 

溶解度: DMSO ≥16mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 405554-55-4

生物活性

 

 

SB-590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration, which is distinct from the previously reported mechanism of action of the multi-kinase inhibitor, BAY43-9006.

Interestingly, selectivity towards B-Raf was shown as SB-590885 inhibited c-Raf with a Ki app of 1.72 ± 0.65 nM. These results showed that SB-590885 was a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 43-9006 (Ki app = 38 nM for mutant B-Raf, 6 nM for c-Raf) and exhibited more selectivity towards B-Raf inhibition. SB-590885 was further profiled against a panel of 48 other human kinases, comprising representatives from all of the main branches of the human kinome. Strikingly, SB-590885 displayed remarkable specificity for B-Raf inhibition, with significant activity measured only against c-Raf and minimal off-target activity.[1][2]

 

 

 

参考文献

Demonstration of a Genetic Therapeutic Index for Tumors by the Kinase Inhibitor BRAF Expressing Oncogenic SB-590885 Denis R. Patrick, Roberta S. Batorsky, et al. Cancer Res 2006;66:11100-11105

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现货,PHA-793887,CAS号:718630-59-2,美国进口,细胞周期(Cell Cycle / Checkpoint) , CDK , CDK 抑制剂和化合物,selleck,S1487

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> CDK >> CDK 抑制剂和化合物 >> PHA-793887http://selleck.cn/pha-793887-S1487.html

技术数据:

分子量(MW): 361.48

化学式:

C19H31N5O2

 

溶解度: DMSO ≥72mg/mL Water <1mg/mL Ethanol ≥72mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 718630-59-2

生物活性

 

 

PHA-793887 is a novel pan-cdk inhibitor, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range. [1]It is inactive against other 34 kinases representative of all kinase families, in particular c-abl, c-kit, lck, and TRKA with IC50>10 mM. It shows anti-proliferative activity against several solid tumor cell lines, with IC50<1 mM. In these cells, it is able to inhibit Rb phosphorylation and expression of S-phase cyclins, such as cyclin A. [1,2]

 

 

 

参考文献

Transcriptional Analysis of an E2F Gene Signature as a Inhibitor Biomarker of Activity of the Cyclin-Dependent Kinase PHA-793887 in Tumor and Skin Biopsies from a Phase I Clinical Study Roberta Bosotti, Marina Ciomei, et al. Mol Cancer Ther 2010;9:1265-1273

Poly ADP ribose polymerase (PARP) inhibitors Rachele Alzani,Olga Pedrini,et al. Experimental Hematology 2010 ;38:259–269

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0 Comments

现货,TG100-115 ,CAS号:677297-51-7,美国进口,PI3K / mTOR / AKT , PI3K , PI3K 抑制剂,selleck,目录号S1352

信号转导通路: PI3K / mTOR / AKT >> PI3K >> PI3K 抑制剂 >> TG100-115http://www.selleck.cn/tg100-115-S1352.html

技术数据:

分子量(MW): 346.34

化学式:

C18H14N6O2

 

溶解度: DMSO ≥9mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 677297-51-7

生物活性

 

 

TG100-115, inhibited PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and -β were relatively unaffected (IC50 values>1 μM). As a gauge of general specificity, TG100-115 was also assayed against a 133 protein kinase panel, none of which was inhibited at IC50 values <1 μM. [ 2,3]

TG100-115 is applied to anti-inflammatory therapy for respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). TG100-115 could reduce inflammation and mucin accumulation.

 

 

 

参考文献

Phosphoinositide 3-kinase γ/δ inhibition limits infarct size after myocardial ischemia/reperfusion injury John Doukas,Wolfgang Wrasidlo,et al. PNAS December 26, 2006;103:19866–19871

Aerosolized Phosphoinositide 3-Kinase γ/δ Inhibitor TG100-115 [3-[2,4-Diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a Therapeutic Candidate for Asthma and Chronic Obstructive Pulmonary Disease John Doukas, Lisa Eide,et al. JPET 2009;328:758–765

 

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现货,AR-42 (HDAC-42),CAS号:935881-37-1,美国进口,HDAC-HSP-Aurora , HDAC ,HDAC 抑制剂,sellek,S2244

信号转导通路:  HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂 >> 

信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂 >> AR-42 (HDAC-42)http://www.selleck.cn/ar-42-hdac-42-S2244.html

技术数据:

分子量(MW): 312.36

化学式:

C18H20N2O3

 

溶解度: DMSO ≥63mg/mL Water <1mg/mL Ethanol ≥63mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 935881-37-1

生物活性

 

 

AR-42 is a novel HDAC inhibitor with an IC50 of 0.61 μM for acute lymphoblastic leukemia (697) cell lines.

In chronic lymphocytic leukemia (CLL) cells, the 48-hr LC50 of AR-42 is 0.76 μM. AR-42 produces dose- and time-dependent acetylation both of histones and tubulin, and induces caspase-dependent apoptosis that is not reduced in the presence of stromal cells. AR-42 significantly reduced leukocyte counts and/or prolonged survival in three separate mouse models of B-cell malignancy without evidence of toxicity. AR-42 has in vitro and in vivo efficacy at tolerable doses. In additon, AR-42 promoted hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. Down-regulation of Kit occurred after AR-42 treatment via inhibition of Kit transcription. [1][2]

 

 

 

参考文献

The novel deacetylase inhibitor AR-42 demonstrates pre-clinical activity in B-cell malignancies in vitro and in vivo. Lucas DM et al. PLoS One. 2010 Jun 3;5(6):e10941.

AR-42, a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit. Lin TY et al. Blood. 2010 May 27;115(21):4217-25.

 

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现货,GSK429286A,CAS号:864082-47-3,美国进口,细胞周期(Cell Cycle / Checkpoint), ROCK, ROCK 抑制剂和化合物,selleck,S1474

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> ROCK >> ROCK 抑制剂和化合物 >> GSK429286Ahttp://www.selleck.cn/gsk429286a-S1474.html

技术数据:

分子量(MW): 432.37

化学式:

C21H16F4N4O2

 

溶解度: DMSO ≥87mg/mL Water ≥87mg/mL Ethanol ≥17mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 864082-47-3

生物活性

 

 

GSK429286A is a cell-permeable, selective Rho-associated kinase (ROCK) inhibitor with an IC50 of 14 nM. Not only was GSK429286A a potent ROCK1 inhibitor, but GSK429286A also possessed exciting selectivity (30-fold) against a panel of 33 kinases, including RSK1 (IC50 = 3.1 μM) and p70S6K (Ic50 = 2.85μM). ROCKs are serine/threonine specific protein kinases which play a crucial role in organization of the actin cytoskeleton. ROCK inhibitors have been found to prevent apoptosis, as well as to enhance the survival and cloning efficiency of dissociated human embryonic stem (ES) cells without affecting their self-renewal properties or pluripotency. Because of GSK429286A

 

 

 

参考文献

Development of Dihydropyridone Indazole Amides as Selective Rho-Kinase Inhibitors Haifeng Cui, Sarah E. Dowdell,et al. J. Med. Chem 2007;50:6-9

Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson’s disease R. Jeremy NICHOLS,Nicolas DZAMKO,et al. Biochem. J 2009;424:47–60

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现货,Vatalanib (PTK787),CAS号212141-51-0,美国进口,:受体酪氨酸激酶(RTK), VEGFR ,VEGFR 抑制剂和化合物,selleck,S1101

信号转导通路: 受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR 抑制剂 >> Vatalanib dihydrochloride (PTK787)http://www.selleck.cn/vatalanib-S1101.html

技术数据:

分子量(MW): 419.73

化学式:

C20H15ClN4•2HCl

 

溶解度: DMSO ≥28mg/mL Water ≥10mg/mL Ethanol ≥6mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 212141-51-0

生物活性

 

 

Vatalanib dihydrochloride (PTK787) is a novel VEGFR and c-Kit tyrosine kinases and angiogenesis inhibitor with IC50 of 0.037, 0.077, 0.27 and 0.73 μM for KDR, Flt-1, Flk and c-Kit, respectively. Measurement of VEGF-induced autophosphorylation of KDR in a double antibody chemiluminescence assay, using either HUVECs or CHO cells transfected with the KDR receptor, showed that vatalanib dihydrochloride (PTK787) inhibits the VEGF-induced phosphorylation with an IC50 of 17 and 34 nM for the HUVECs and CHO cells , respectively. Selective inhibition of VEGFRs by vatalanib dihydrochloride (PTK787)leads to inhibition of primary tumor growth and development of metastases in murine renal cell carcinoma. Vatalanib dihydrochloride (PTK787) caused no obvious side effects in the RENCA model . Vatalanib dihydrochloride (PTK787) causes significant anti-arthritic effects in models of rheumatoid arthritis. [1][2][3]

 

 

 

参考文献

PTK787/ZK 222584, a Novel and Potent Inhibitor of Vascular Impairs Endothelial Growth Factor Receptor Tyrosine Kinases,Vascular Endothelial Growth Factor-induced Responses and Tumor Growth after Oral Administration Guido Bold, Elizabeth Buchdunger, et al. Cancer Res 2000;60:2178-2189

Effects of PTK787/ZK 222584, a Specific Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases, on Primary Tumor, Metastasis, Vessel Density, and Blood Flow in a Murine Renal Cell Carcinoma Model Joachim Drevs, Inga Hofmann,et al. Cancer Res 2000;60:4819-4824

Angiogenesis inhibition by the novel VEGF receptor tyrosine kinase inhibitor, PTK787/ZK222584, causes significant anti-arthritic effects in models of rheumatoid arthritis K. Grosios,J.Wood,et al. Inflamm. res 2004;53:133–142

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现货,Pelitinib (EKB-569) ,CAS号:257933-82-7,美国进口,受体酪氨酸激酶(RTK) , EGFR , EGFR 抑制剂和化合物,selleck,S1392

信号转导通路: 受体酪氨酸激酶(RTK) >> EGFR >> EGFR 抑制剂和化合物 >> Pelitinib (EKB-569)http://selleck.cn/pelitinib-S1392.html

技术数据:

分子量(MW): 467.92

化学式:

C24H23ClFN5O2

 

溶解度: DMSO ≥13mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 257933-82-7

生物活性

 

 

Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. Pelitinib irreversibly binds covalently to epidermal growth factor receptors (EGFR) ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these receptors. Pelitinib inhibits EGF-induced phosphorylation of EGF-R and the growth of tumors that overexpress EGF-R in animal models.[1][2]

 

 

 

参考文献

Phase I Pharmacokinetic/Pharmacodynamic Study of EKB-569, an Irreversible Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in Combination with Irinotecan, 5-Fluorouracil, and Leucovorin (FOLFIRI) in First-Line Treatment of Patients with Metastatic Colorectal Cancer Josep Tabernero, Claus-Henning Köhne, et al. Clin Cancer Res 2008;14:215-223

Synthesis and Structure-Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2) Allan Wissner, Elsebe Overbeek,et al. J. Med. Chem. 2003;46, 49-63

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现货,PP242,CAS号:1092351-67-1,美国进口,PI3K / mTOR / AKT, mTOR , mTOR 抑制剂和化合物,selleck,S2218

信号转导通路: PI3K / mTOR / AKT >> mTOR >> mTOR 抑制剂和化合物 >> PP242http://www.selleck.cn/pp242-S2218.html

技术数据:

分子量(MW): 308.34

化学式:

C16H16N6O

 

溶解度: DMSO ≥62mg/mL Water <1mg/mL Ethanol ≥34mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1092351-67-1

生物活性

 

 

PP242 is a novel potent and selective mTOR inhibitor with an IC50 of 8 nM. PP242 also shows residual (micromolar) activity against panel of tyrosine kinases. But PP242 was much less active against other PI3K family members with IC50 of 2, 2.2, 0.1, 1.3 and 0.41 μM for p110α, p110β, p110δ, p110γ and DNA-PK, respectively.

PP242 inhibits other PI 3-Kinases only at much higher concentrations. PP242, but not rapamycin, causes death of mouse and human leukemia cells. In vivo, PP242 delays leukemia onset and augments the effects of the current front-line tyrosine kinase inhibitors more effectively than does rapamycin. PP242 was also more effective than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma cells. In addition, PP242 was an effective agent against primary multiple myeloma cells in vitro and growth of 8226 cells in mice. Knockdown of the TORC2 complex protein, rictor, was deleterious to multiple myeloma cells further supporting TORC2 as the critical target for PP242. [1][2][3]

 

 

 

参考文献

Targeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases Beth Apsel,Jimmy A. Blair,et al. Nat Chem Biol 2008 November;4(11): 691–699

Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor Matthew R Janes,Jose J Limon,et al. nature medicine february 2010 ;16:205-214

Targeting TORC2 in multiple myeloma with a new mTOR kinase inhibitor Bao Hoang, Patrick Frost,et al. Blood 2010;116: 4560-4568

 

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0 Comments

现货,GSK690693,CAS号:937174-76-0,美国进口,PI3K / mTOR / AKT , AKT,AKT 抑制剂和化合物,selleck,S1113

信号转导通路: PI3K / mTOR / AKT >> AKT >> AKT 抑制剂 >> GSK690693http://www.selleck.cn/gsk690693-S1113.html

技术数据:

分子量(MW): 425.48

化学式:

C21H27N7O3

 

溶解度: DMSO ≥39mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 937174-76-0

生物活性

 

 

GSK690693 is an aminofurazan-derived,novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms(inhibits Akt kinases 1, 2, and 3 with IC50 values of 2, 13, and 9 nM respectively)versus the majority of kinases in other families; however, it does inhibit additional members of the AGC kinase family. [1,2]

 

GSK690693 inhibited proliferation and induced apoptosis in a subset of tumor cells with potency consistent with intracellular inhibition of Akt kinase activity. [1]

 

Daily administration of GSK690693 produced significant antitumor activity in mice bearing established human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts. [1]

 

 

 

参考文献

Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity Dirk A. Heerding, Derek R. Duckett, et al. Cancer Res 2008;68:2366-2374

Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase Dirk A. Heerding,Nelson Rhodes,et al. J. Med. Chem 2008;51: 5663–5679

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现货,JNJ-7706621, CAS号:443797-96-4,美国进口,细胞周期(Cell Cycle / Checkpoint) , CDK , CDK 抑制剂 ,selleck,目录号S1249

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> CDK >> CDK 抑制剂和化合物 >> JNJ-7706621http://www.selleck.cn/jnj-7706621-S1249.html

技术数据:

分子量(MW): 394.36

化学式:

C15H12F2N6O3S

 

溶解度: DMSO ≥79mg/mL Water <1mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 443797-96-4

生物活性

 

 

JNJ-7706621 is a dual cyclin-dependent kinases and aurora kinases inhibitor with IC50 of 9 and 11 nM for CDK1/Cyclin B and aurora-A, respectively. JNJ-7706621 blocked proliferation of cancer cells regardless of their p53, retinoblastoma or P-glycoprotein status and induced cell death by activating apoptosis. JNJ-7706621 was about 10 fold less effective at inhibiting proliferation of normal cells. Flow cytometric analysis of DNA content in human tumor cells showed that JNJ-7706621 delayed progression through G1 and arrested the cell cycle at the G2/M phase. JNJ-7706621 also decreased CDK1 kinase activity, altered CDK1 phosphorylation status and blocked signaling to downstream substrates of CDKs. Additional cellular effects including endoreduplication and reduced histone H3 phosphorylation were also observed due to inhibition of Aurora kinase. JNJ-7706621 demonstrated significant inhibition of tumor growth in a variety of tumor types in nude mice xenograft models. In vitro cell proliferation assays IC50 (μM): HeLa (IC50=0.286), HCT-116 (IC50=0.189), PC3 (IC50=0.112). JNJ-7706621 is not affected by P-glycoprotein. [1][2][3]

 

 

 

参考文献

The In vitro and In vivo Effects of JNJ-7706621: A Dual Inhibitor of Cyclin-Dependent Kinases and Aurora Kinases Catherine A. Rugg, Robert H. Gruninger, et al. Cancer Res 2005;65:9038-9046

Preclinical profile of JNJ-7706621: A dual cyclin dependent kinase and aurora kinase inhibitor Stuart L. Emanuel,et al. Proc Amer Assoc Cancer Res. 2006;47

Evaluation of the CDK inhibitor JNJ-7706621 as a targeted antitumor agent Stuart L. Emanuel,et al. Proc Amer Assoc Cancer Res. 2004;45

 

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现货,Thiazovivin,CAS号:1226056-71-8,美国进口,细胞周期(Cell Cycle / Checkpoint) , ROCK , ROCK 抑制剂,selleck,S1459

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> ROCK >> ROCK 抑制剂 >> Thiazovivinhttp://www.selleck.cn/thiazovivin-S1459.html

技术数据:

分子量(MW): 311.36

化学式:

C15H13N5OS

 

溶解度: DMSO ≥62mg/mL Water <1mg/mL Ethanol ≥5mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1226056-71-8

生物活性

 

 

Thiazovivin is a compound which dramatically improves the survival of hESCs upon trypsinization. Thiazovivin dramatically improves the survival of hESCs upon trypsinization. In combination with ALK5 (TGFβ receptor) inhibitor SB-431542 and MEK inhibitor PD-0325901, thiazovivin promotes the transformation of fibroblasts into stem cells with a 200-fold efficiency over the classic method. [1]

 

 

 

参考文献

Effect of Fasudil HCl, a protein kinase inhibitor, on cerebral vasospasm. Shibuya M et al. Acta Neurochir Suppl. 2001;77:201-4.

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0 Comments

现货,LY2603618 (IC-83),CAS号:911222-45-2,美国进口,细胞周期(Cell Cycle / Checkpoint) ,CHK ,CHK 抑制剂和化合物,selleck,目录号S2626

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> CHK >> CHK 抑制剂 >> LY2603618 (IC-83)http://www.selleck.cn/ly2603618-ic-83-S2626.html

技术数据:

分子量(MW): 436.3

化学式:

C18H22BrN5O3

 

溶解度: DMSO ≥21mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 911222-45-2

生物活性

 

 

LY2603618 (IC-83) is a highly selective Chk 1 inhibitor with potential antitumor activity. LY2603618 (IC-83) binds to and inhibits the activity of chk1, which may prevent the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. Chk1, an ATP-dependent serine-threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk1 is overexpressed by a variety of cancer cell types. [1][2]

 

 

 

参考文献

New insights into checkpoint kinase 1 in the DNA damage response signaling network. Dai Y et al. Clin Cancer Res. 2010 Jan 15;16(2):376-83.

http://www.springer.com/biomed/cancer/book/978-1-60761-177-6 http://www.springer.com/biomed/cancer/book/978-1-60761-177-6 ;

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0 Comments

现货,AZD8330,CAS号:869357-68-6,美国进口,MAPK , MEK , MEK 抑制剂,selleck,S2134

信号转导通路: MAPK >> MEK >> MEK 抑制剂和化合物 >> AZD8330http://www.selleck.cn/azd8330-arry-424704-S2134.html

技术数据:

分子量(MW): 461.23

化学式:

C16H17FIN3O4

 

溶解度: DMSO ≥92mg/mL Water <1mg/mL Ethanol ≥92mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 869357-68-6

生物活性

 

 

AZD8330 is an orally active, selective MEK inhibitor with an IC50 of 7 nM. AZD8330 has potential antineoplastic activity. AZD8330 specifically inhibits mitogen- activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. Constitutive activation of this pathway has been implicated in many cancers. [1][2]

 

 

 

参考文献

From basic research to clinical development of MEK1/2 inhibitors for cancer therapy Christophe Frémin, Sylvain Meloche Journal of Hematology & Oncology 2010;3:8

 

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0 Comments

现货,PD98059,CAS号:167869-21-8,美国进口,MAPK , MEK, MEK 抑制剂和化合物,selleck,目录号S1177

信号转导通路: MAPK >> MEK >> MEK 抑制剂 >> PD98059http://www.selleck.cn/pd-98059-S1177.html

技术数据:

分子量(MW): 267.28

化学式:

C16H13NO3

 

溶解度: DMSO ≥32mg/mL Water <1mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 167869-21-8

生物活性

 

 

PD 98059 is a highly selective inhibitor of MEK1 and MEK2 with IC50 values of 4 µM and 50 µM respectively[1–3] . PD98059 does not inhibit activation of other highly related dual-specificity protein kinases or the activity of over 18 other Ser/Thr protein kinases. At concentrations up to 100 µM, PD98059 does not inhibit activation of MKK3 or SEK (MKK4) as determined by measuring phosphorylation at its activation site. [1–3]

 

 

 

参考文献

Regional Selective Neuronal Degeneration after Protein Phosphatase Inhibition in Hippocampal Slice Cultures: Evidence for a MAP Kinase-Dependent Mechanism Elise Runden,Per O. Seglen,et al. The Journal of Neuroscience September 15, 1998;18(18):7296–7305

Mitogen-Activated Protein Kinases (Erk1,2) Phosphorylate Lys-Ser-Pro (KSP) Repeats in Neurofilament Proteins NF-H and NF-M Veeranna,Niranjana D. Amin,et al. The Journal of Neuroscience June 1, 1998;18(11):4008–4021

Nerve Growth Factor Activates Extracellular Signal-Regulated Kinase and p38 Mitogen-Activated Protein Kinase Pathways To Stimulate CREB Serine 133 Phosphorylation JUN XING,JON M. KORNHAUSER,et al. MOLECULAR AND CELLULAR BIOLOGY Apr. 1998;18:1946–1955

 

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0 Comments

现货,CX-4945 ,CAS号:1009820-21-6,美国进口,TGF-beta / smad , PKC ,PKC 抑制剂,selleck,S2248

信号转导通路: TGF-beta / smad >> PKC >> PKC 抑制剂 >> CX-4945http://selleck.cn/cx-4945-S2248.html

技术数据:

分子量(MW): 349.77

化学式:

C19H12ClN3O2

 

溶解度: DMSO ≥70mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1009820-21-6

生物活性

 

 

CX-4945 is a potent and selective ATP-competitive small molecule protein kinase CK2 inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. CX-4945 has broad spectrum anti-proliferative activity in multiple cancer cell lines. The antiproliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 (CX 4945; Silmitasertib) was evidenced by dephosphorylation of Akt on the CK2-specific S129 site and the canonical S473 and T308 regulatory sites. CX-4945 suppresses Akt signaling and inhibits proliferation of HUVEC Cells. CX-4945 caused cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells. Collectively, CX-4945 inhibits pro-angiogenic CK2 signaling in vitro and in vivo. [1][2][3]

 

 

 

参考文献

CX-4945, an Orally Bioavailable Selective Inhibitor of Protein Kinase CK2, Inhibits Prosurvival and Angiogenic Signaling and Exhibits Antitumor Efficacy Denis Drygin, Nicole Streiner, et al. Cancer Res 2010;70:10288-10298

Structural basis of CX-4945 binding to human protein kinase CK2 Andrew D. Ferguson, Payal R. Sheth,et al. FEBS Letters 2011;585:104–110

Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the Treatment of Cancer Fabrice Pierre,PeterC.Chua,et al. J. Med. Chem 2011;54:635–654

 

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0 Comments

现货,AZD8931,CAS号:848942-61-0,美国进口, 受体酪氨酸激酶(RTK) , HER2 , HER2 抑制剂

信号转导通路: 受体酪氨酸激酶(RTK) >> HER2 >> HER2 抑制剂 >> AZD8931http://www.selleck.cn/azd8931-S2192.html

技术数据:

分子量(MW): 473.93

化学式:

C23H25ClFN5O3

 

溶解度: DMSO ≥95mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 848942-61-0

生物活性

 

 

AZD8931 is a novel potent reversible small molecule epidermal growth factor receptor, ERBB2 (HER2) and ERBB3 inhibitor with an IC50 of 4, 3, 4 nM, respectively. In proliferation assays, AZD8931 was significantly more potent than gefitinib or lapatinib in specific squamous cell carcinoma of the head and neck and non-small cell lung carcinoma cell lines. In vivo, AZD8931 inhibited xenograft growth in a range of models while significantly affecting EGFR, erbB2, and erbB3 phosphorylation and downstream signaling pathways, apoptosis, and proliferation. It has a unique pharmacologic profile providing equipotent inhibition of EGFR, erbB2, and erbB3 signaling and showing greater antitumor activity than agents with a narrower spectrum of erbB receptor inhibition in specific preclinical models. [1][2][3]

 

 

 

参考文献

AZD8931, an Equipotent, Reversible Inhibitor of Signaling by Epidermal Growth Factor Receptor, ERBB2 (HER2), and ERBB3: A Unique Agent for Simultaneous ERBB Receptor Blockade in Cancer Teresa Klinowska, Georgina Speake, et al. Clin Cancer Res 2010;16:1159-1169

http://www.cancer.gov/drugdictionary/?CdrID=593099 http://www.cancer.gov/drugdictionary/?CdrID=593099 ;

Characterization of AZD8931, a potent reversible small molecule inhibitor against epidermal growth factor receptor (EGFR), erythroblastic leukemia viral oncogene homolog 2 (HER2) and 3 (HER3) with a unique and balanced pharmacological profile G. Speake et al. Journal of Clinical Oncology May 20, 2009;27(15S)

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现货, JNJ 26854165,CAS号:881202-45-5,美国进口, 细胞凋亡(Apoptosis) , p53 , p53 抑制剂和化合物,selleck,S1172

信号转导通路: 细胞凋亡(Apoptosis) >> p53 >> p53 抑制剂和化合物 >> JNJ 26854165http://selleck.cn/jnj-26854165-S1172.html

技术数据:

分子量(MW): 328.41

化学式:

C21H20N4

 

溶解度: DMSO ≥66mg/mL Water <1mg/mL Ethanol ≥2mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 881202-45-5

生物活性

 

 

JNJ-26854165 is an orally bioavailable, small-molecule HDM2 antagonist with potential antineoplastic activity. JNJ-26854165 inhibits the binding of the HDM2–p53 complex to the proteasome, blocking the degradation of p53; p53 signaling and p53-mediated induction of tumor cell apoptosis may thus be restored. In addition to p53, degradation of other HDM2 client proteins may be inhibited. HDM2 (human homolog of double minute 2), a zinc finger protein, is a negative regulator of the p53 pathway; often overexpressed in cancer cells, this oncoprotein has been implicated in cancer cell proliferation and survival. [1][2]

 

 

 

参考文献

A first-in-class HDM2-inhibitor (JNJ-26854165) in phase I development shows potent activity against multiple myeloma (MM) cells in vitro and ex vivo T. Stühmer et.al. ASCO Annual Meeting 2008;Vol 26, No 15S

HDM2 antagonist JNJ-26854165 http://www.cancer.gov/drugdictionary/?CdrID=596734 ;

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物品的等)将不予退换。

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0 Comments

现货,MG-132,CAS号:133407-82-6,美国进口,蛋白酶体(Proteases) , Proteasome ,Proteasome 抑制剂和化合物,selleck,目录号S2619

信号转导通路: 蛋白酶体(Proteases) >> Proteasome >> Proteasome 抑制剂 >> MG-132http://www.selleck.cn/mg-132-S2619.html

技术数据:

分子量(MW): 475.62

化学式:

C26H41N3O5

 

溶解度: DMSO ≥95mg/mL Water <1mg/mL Ethanol ≥95mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 133407-82-6

生物活性

 

 

MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50 of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively. The Ki of MG132 is 4 nM. MG132 inhibits TNF-α-induced NF-κB activation and IκBα degradation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132 induces neurite outgrowth in PC12 cells and has anticancer properties in vitro. MG132 reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. [1][2][3]

 

 

 

参考文献

Differential Inhibition of Calpain and Proteasome Activities by Peptidyl Aldehydes of Di-Leucine and Tri-Leucine Satoshi Tsubuki,Yumiko Saito,et al. J. Biochem 1996;119:, 572-576

http://en.wikipedia.org/wiki/MG132 http://en.wikipedia.org/wiki/MG132 ;

The protease inhibitor, MG132, blocks maturation of the amyloid precursor protein Swedish mutant preventing cleavage by beta-Secretase. Steinhilb ML et al. J BiolChem. 2001 Feb 9;276(6):4476-84.

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现货,LY2784544,CAS号:1229236-86-5,美国进口,JAK / STAT , JAK, JAK 抑制剂和化合物,目录号S2179

信号转导通路:  JAK / STAT >> JAK >> JAK 抑制剂和化合物 >> 

信号转导通路: JAK / STAT >> JAK >> JAK 抑制剂和化合物 >> LY2784544http://www.selleck.cn/ly2784544-S2179.html

技术数据:

分子量(MW): 469.94

化学式:

C23H25ClFN7O

 

溶解度: DMSO ≥94mg/mL Water <1mg/mL Ethanol ≥9mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1229236-86-5

生物活性

 

 

LY2784544 is a small molecule selective mutant JAK2 kinase inhibitor with an IC50 of 68 nM. The antiproliferative activity of LY2784544 and its ability to induce apoptosis were examined by Celltiter-Glo Cell Viability and Caspase-Glo 3/7 Apoptosis Assays, respectively. In the in vitro tests using Ba/F3 cells expressing either wild type or V617F mutant JAK2, it potently inhibited the JAK2 V617F-STAT5 signaling at a concentration that was 41-fold lower than that required to inhibit IL-3-activated wild type JAK2-STAT5 signaling (IC50 = 0.055 µM for JAK2 V617F vs. 2.26 µM for WT JAK2). Similarly in the proliferation assay, LY2784544 selectively inhibited the JAK2 V617F-driven cell proliferation (IC50= 0.068 µM). Inhibition of JAK2 V617F signaling correlated well with the induction of apoptosis (EC50= 0.113 µM) in Ba/F3 cell model. [1]

 

 

 

参考文献

New drugs for the treatment of myelofibrosis. Mesa RA. Curr Hematol Malig Rep. 2010 Jan;5(1):15-21.

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现货 ,SGI-1776 free base ,CAS号: 1025065-69-3,美国进口,JAK / STAT , Pim , Pim 抑制剂

信号转导通路: JAK / STAT >> Pim >> Pim 抑制剂 >> SGI-1776 free basehttp://www.selleck.cn/sgi-1776-S2198.html

技术数据:

分子量(MW): 405.42

化学式:

C20H22F3N5O

 

溶解度: DMSO ≥81mg/mL Water <1mg/mL Ethanol ≥81mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1025065-69-3

生物活性

 

 

SGI-1776 free base is a selective Pim family kinase inhibitor with IC50 of 7 ± 1.8, 363 ± 27.6 and 69 ± 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively.

SGI-1776 is a member of the imidazo[1,2-b]pyridazine chemical class, was selected for its ability to exploit an extended ATP-binding and solvent pocket, thereby making it a selective Pim family kinase inhibitor. Extensive biochemical characterization of SGI-1776 confirmed its specificity for the three isoforms of the Pim family. SGI-1776 is a fairly selective inhibitor of the Pim kinases and can cause a reduction in prostate cancer cell viability and alter overall cytotoxic responses to taxanes. SGI-1776 can disrupt cell cycle progression, induce apoptosis, promote taxane sensitivity, and overcome acquired chemoresistance by inhibiting MDR1 activity in specific prostate cancer models. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. SGI-1776 exhibited inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50= 34 nM). [1][2]

 

 

 

参考文献

Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells Lisa S. Chen, Sanjeev Redkar,et al. Blood 2009;114: 4150-4157

Pharmacologic inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes Patricia Y.B. Ng, Amanda Hodge, et al. Mol Cancer Ther 2009;8:2882-2893

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0 Comments

现货 ,SGI-1776 free base ,CAS号: 1025065-69-3,美国进口,JAK / STAT , Pim , Pim 抑制剂

信号转导通路: JAK / STAT >> Pim >> Pim 抑制剂 >> SGI-1776 free basehttp://www.selleck.cn/sgi-1776-S2198.html

技术数据:

分子量(MW): 405.42

化学式:

C20H22F3N5O

 

溶解度: DMSO ≥81mg/mL Water <1mg/mL Ethanol ≥81mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1025065-69-3

生物活性

 

 

SGI-1776 free base is a selective Pim family kinase inhibitor with IC50 of 7 ± 1.8, 363 ± 27.6 and 69 ± 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively.

SGI-1776 is a member of the imidazo[1,2-b]pyridazine chemical class, was selected for its ability to exploit an extended ATP-binding and solvent pocket, thereby making it a selective Pim family kinase inhibitor. Extensive biochemical characterization of SGI-1776 confirmed its specificity for the three isoforms of the Pim family. SGI-1776 is a fairly selective inhibitor of the Pim kinases and can cause a reduction in prostate cancer cell viability and alter overall cytotoxic responses to taxanes. SGI-1776 can disrupt cell cycle progression, induce apoptosis, promote taxane sensitivity, and overcome acquired chemoresistance by inhibiting MDR1 activity in specific prostate cancer models. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. SGI-1776 exhibited inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50= 34 nM). [1][2]

 

 

 

参考文献

Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells Lisa S. Chen, Sanjeev Redkar,et al. Blood 2009;114: 4150-4157

Pharmacologic inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes Patricia Y.B. Ng, Amanda Hodge, et al. Mol Cancer Ther 2009;8:2882-2893

客户反馈数据

Mean IL-8 concentrations determined by ELISA of the supernatants of HeLa cells infected with wild-type Salmonella. Kinase inhibitors are indicated on the x axis, and the target families of the inhibitors are indicated above each column. CEC, chelerythrine; Pim Inh, Pim-1 inhibitor 2. Inhibitors that significantly affected IL-8 production relative to the control (P < 0.05, Bonferroni post hoc test from one-way ANOVA) are indicated with an asterisk. Relative cell viability is also shown, as determined by reduction of XTT by viable cells. A450, absorbance at 450 nm.

如果需要长期保存,请于零下二十度低温保存。

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特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20 ° C ,抗体及蛋白等产品建议-60℃。抑制剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。

 

 

 

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0 Comments

现货,AG14361,CAS号:328543-09-5,美国进口,细胞周期(Cell Cycle / Checkpoint),PARP, PARP 抑制剂和化合物,selleck,S2178

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> PARP >> PARP 抑制剂 >> AG14361http://selleck.cn/ag14361-S2178.html

技术数据:

分子量(MW): 320.39

化学式:

C19H20N4O

 

溶解度: DMSO ≥21mg/mL Water <1mg/mL Ethanol ≥12mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 328543-09-5

生物活性

 

 

AG14361 is a potent poly(ADP-ribose) polymerase (PARP-1) inhibitor with a GI50 of 10.9 µM. It caused a >3-fold sensitization of PARP-1+/+ cells to topotecan compared with a <1.4-fold sensitization in PARP-1−/− cells. In human leukemia K562 cells, AG14361 caused a 2-fold sensitization to camptothecin-induced cytotoxicity. AG14361 did not affect the cellular activity of topo I as determined by measurement of cleavable complexes and topo I relaxation activity, showing that sensitization was not due to topo I activation. [1][2][3]

 

 

 

参考文献

Anticancer Chemosensitization and Radiosensitization by the Novel Poly(ADP-ribose) Polymerase-1 Inhibitor AG14361 Christopher R. Calabrese, Robert Almassy,et al. Journal of the National Cancer Institute January 7, 2004;96:56-67

The Novel Poly(ADP-Ribose) Polymerase Inhibitor, AG14361,Sensitizes Cells to Topoisomerase I Poisons by Increasing the Persistence of DNA Strand Breaks Elaine Willmore, Caroline A. Austin, et al. Clin Cancer Res 2005;11:8449-8457

Novel Poly(ADP-ribose) Polymerase-1 Inhibitor, AG14361,Restores Sensitivity to Temozolomide in Mismatch Repair-Deficient Cells Lan-Zhen Wang, Anthie Yiakouvaki, et al. Clin Cancer Res 2004;10:881-889

客户反馈数据

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0 Comments

现货,CYC116,CAS号:693228-63-6,美国进口, HDAC-HSP-Aurora , Aurora Kinase , Aurora Kinase 抑制剂,selleck,S1171

信号转导通路: HDAC-HSP-Aurora >> Aurora Kinase >> Aurora Kinase 抑制剂 >> CYC116http://www.selleck.cn/cyc116-S1171.html

技术数据:

分子量(MW): 368.46

化学式:

C18H20N6OS

 

溶解度: DMSO ≥24mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 693228-63-6

生物活性

 

 

CYC116 is an orally bioavailable,small molecule Aurora kinase/VEGFR2 inhibitor with antineoplastic activity. CYC116 inhibits Aurora kinases A and B and VEGFR2, resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis. [1]

CYC116 has a unique target profile involving both cell cycle and angiogenesis inhibition mechanisms. In preclinical studies, it demonstrated antitumor activity in both solid tumors and hematological cancers.

 

 

 

参考文献

http://www.cancer.gov/drugdictionary/?CdrID=566443 http://www.cancer.gov/drugdictionary/?CdrID=566443 ;

Cyclacel submits IND of CYC116, an Aurora kinase and VEGRF2 inhibitor to treat cancer Medical Letter on the CDC and FDA January 14th, 2007;

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0 Comments

现货,GSK1120212 (JTP-74057) ,CAS号: 871700-17-3,美国进口, MAPK , MEK , MEK 抑制剂,selleck,S2637

信号转导通路: MAPK >> MEK >> MEK 抑制剂 >> GSK1120212 (JTP-74057)http://selleck.cn/gsk1120212-jtp-74057-S2673.html

技术数据:

分子量(MW): 615.39

化学式:

C26H23FIN5O4

 

溶解度: DMSO ≥6mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 871700-17-3

生物活性

 

 

GSK1120212 (JTP-74057) is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. [1] GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. After treatment of GSK1120212 (JTP-74057), it led to the growth inhibition and upregulate p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines tested. In nude animal mice studies, JTP-74057 inhibited tumor growth of HT-29 and COLO205 xenografts when GSK1120212 (JTP-74057) was daily oral administered for 14 days. GSK1120212 (JTP-74057) showed an additive or a synergistic action in combination with the standard-of-care agents, 5-fluorouracil, oxaliplatin or SN-38. Sensitivity to JTP-74057-induced apoptosis may be an important factor for the estimation of in vivo efficacy, and sensitivity was enhanced by an Akt inhibitor. [2] GSK1120212 (JTP-74057) is originally developed by GlaxoSmithKline and is recruiting for phase I clinical trials for the treatment of solid tumors.

 

 

 

参考文献

Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo Yamaguchi T et al. Int J Oncol. 2011 Jul;39(1):23-31.

GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Gilmartin AG et al. Clin Cancer Res. 2011 Mar 1;17(5):989-1000.

客户反馈数据

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4、Selleck目前只支持商品一换一服务,换货时无法加定商品。

5、如您购买商品时Selleck上海办事处已向您提供发票,则办理退货或订单金额发生变更的换货时,请将发票随商品一同返还给Selleck上海办事处赛导通生物科技(上海)有限公司,请您妥善保管发票,如发票丢失,将无法办理退换货。

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现货,ZM-447439, CAS号:331771-20-1,美国进口,HDAC-HSP-Aurora , Aurora Kinase ,Aurora Kinase 抑制剂和化合物,selleck,S1103

信号转导通路: HDAC-HSP-Aurora >> Aurora Kinase >> Aurora Kinase 抑制剂和化合物 >> ZM-447439http://selleck.cn/zm-447439-S1103.html

技术数据:

分子量(MW): 513.59

化学式:

C29H31N5O4

 

溶解度: DMSO ≥103mg/mL Water <1mg/mL Ethanol ≥48mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 331771-20-1

生物活性

 

 

ZM-447439 is a potent and selective Aurora B kinase inhibitor with an IC50 of 50 nM, 1 μM and 250 nM for Aurora B, A and C, respectively. Other kinases such as Cdk1 and PLK1 are not inhibited (up to 10 mM). Cells treated with ZM-447439 progress through interphase, enter mitosis and assemble bipolar spindles but chromosome alignment, segregation and cytokinesis all fail. Mitotic Aurora kinases are essential for accurate chromosome segregation during cell division. Forced overexpression of Aurora kinase results in centrosome amplification and multipolar spindles, causing aneuploidy, a hallmark of cancer. ZM447439 does not interfere with other kinases when used up to 5 µM. ZM447439 dose-dependently inhibited proliferation of all three cell lines (BON, QGP-1 and MIP-101) with IC50 values in the nanomolar to low micromolar range. Moreover, aurora kinase inhibition by ZM447439 potently induced apoptosis, which was accompanied by DNA fragmentation and caspase 3 and 7 activation. [1][2][3]

 

 

 

参考文献

ZM 447439 inhibition of aurora kinase induces Hep2 cancer cell apoptosis in three-dimensional culture Zi-Jie Long,Jie Xu,et al. Cell Cycle 15 May 2008;7:10, 1473-1479

Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2,and Cenp-E to kinetochores Claire Ditchfield,Victoria L. Johnson,et al. The Journal of Cell Biology 2003;161:267–280

Discovery of Novel and Potent Thiazoloquinazolines as Selective Aurora A and B Kinase Inhibitors Georges Pasquet,Christine Lambert-van der Brempt,et al. J. Med. Chem 2006;49:955-970

 

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现货,LY2228820 ,CAS号:862507-23-1,美国进口, MAPK , p38 MAPK, p38 MAPK 抑制剂和化合物,selleck,S1494

信号转导通路: MAPK >> p38 MAPK >> p38 MAPK 抑制剂和化合物 >> LY2228820http://selleck.cn/ly2228820-S1494.html

技术数据:

分子量(MW): 612.74

化学式:

C24H29FN6.2CH4O3S

 

溶解度: DMSO ≥35mg/mL Water ≥123mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: -20℃ 2 years

CAS号: 862507-23-1

生物活性

 

 

LY2228820 is a novel and potent p38MAPK inhibitor: in vitro kinase enzyme activity showed that the IC50 for p38αMAPK and p38βMAPK were 7 nM and 3 nM, respectively, while that for p38δMAPK, p38γMAPK and a panel of 172 additional kinases was more than 20 µM. Phosphorylation of MAPKAPK2 and/or HSP27, down stream targets of p38MAPK, was significantly inhibited by LY in both MM cell lines and LT-BMSCs. [1]

 

 

 

参考文献

p38 mitogen-activated protein kinase inhibitor LY2228820 enhances bortezomib-induced cytotoxicity and inhibits osteoclastogenesis in multiple myeloma; therapeutic implications Kenji Ishitsuka,Teru Hideshima,et al. British Journal of Haematology 2008;141:598–606

 

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现货,INO-1001, CAS号:3544-24-9,美国进口,细胞周期(Cell Cycle / Checkpoint) ,PARP,PARP 抑制剂和化合物,selleck,S1132

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> PARP >> PARP 抑制剂 >> INO-1001http://www.selleck.cn/ino-1001-S1132.html

技术数据:

分子量(MW): 136.15

化学式:

C7H8N2O

 

溶解度: DMSO ≥27mg/mL Water ≥27mg/mL Ethanol ≥27mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 3544-24-9

生物活性

 

 

INO-1001 is an isoindolinone derivative and potent inhibitor of the nuclear enzyme PARP (poly (ADP-ribose) polymerase) with chemosensitization and radiosensitization properties[1,2]. INO-1001 inhibits PARP, which may result in inhibition of tumor cell DNA repair mechanisms and, so, tumor cell resistance to chemotherapy and radiation therapy. PARP enzymes are activated by DNA breaks and have been implicated in the repair of DNA single-strand breaks (SSB). In addition,INO-1001 improves the recovery of myocardial and endothelial function after hypothermic cardiac arrest and reduces pulmonary injury associated with extracorporal circulation.[3,4,5]

 

 

 

参考文献

Radiosensitization of human and rodent cell lines by INO-1001,a novel inhibitor of poly(ADP-ribose) polymerase William A. Brock,Luka Milas,etal. Cancer Letters 2004;205:155–160

INO-1001, a novel inhibitor of poly(ADP-ribose) polymerase,enhances tumor response to doxorubicin Kathryn A. Mason,David Valdecanas,et al. Invest New Drugs 2008;26:1–5

Beneficial effects of PJ34 and INO-1001, two novel water-soluble poly(ADP-ribose) polymerase inhibitors, on the consequences of traumatic brain injury in rat Valerie C. Bessona,Zsuzsanna Zsengeller,et al. Brain Research 2005;1041:149– 156

In vitro effect of the potent poly(ADP-ribose) polymerase (PARP) inhibitor INO-1001 alone and in combination with aspirin, eptifibatide, tirofiban,enoxaparin or alteplase on haemostatic parameters Orsolya Tóth , Csaba Szabó,et al Life Sciences 2006;79:317–323

客户反馈数据

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0 Comments

现货,BIX 02188 ,CAS号:1094614-84-2,美国进口,MAPK, MEK, MEK 抑制剂,selleck,S1530

信号转导通路: MAPK >> MEK >> MEK 抑制剂 >> BIX 02188http://selleck.cn/bix-02188-S1530.html

技术数据:

分子量(MW): 426.51

化学式:

C26H26N4O2

溶解度: DMSO ≥43mg/mL Water <1mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1094614-84-2

生物活性

 

BIX02188 is a MEK5-selective inhibitor with an IC50 of 0.8 ± 1.0 μM. It completely reversed the inhibitory effects of flow. [1] The physiological roles of ERK5 in neuronal cells have not been clarified. One reason was the lack of a selective ERK5 pharmacological inhibitor until the novel selective MEK5/ERK5 inhibitors BIX02188 and BIX02189. [2]

 

参考文献

Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells Lingli Li, Revati J. Tatake,et al. Biochem Biophys Res Commun 2008 May 23;370(1): 159–163

The Signaling Pathway Leading to Extracellular Signal-Regulated Kinase 5 (ERK5) Activation via G-Proteins and ERK5-Dependent Neurotrophic Effects Yutaro Obara and Norimichi Nakahata Mol Pharmacol 2010;77:10–16

The Signaling Pathway Leading to Extracellular Signal-Regulated Kinase 5 (ERK5) Activation via G-Proteins and ERK5-Dependent Neurotrophic Effects Yutaro Obara and Norimichi Nakahata Mol Pharmacol 2010;77:10–16

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0 Comments

现货, MK-1775 ,CAS号:955365-80-7,美国进口,细胞周期(Cell Cycle / Checkpoint), Wee1,Wee1 抑制剂,selleck,S1525

信号转导通路:  细胞周期(Cell Cycle / Checkpoint) >> Wee1 >> Wee1 抑制剂 >> 

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> Wee1 >> Wee1 抑制剂 >> MK-1775http://selleck.cn/mk-1775-S1525.html

技术数据:

分子量(MW): 500.6

化学式:

C27H32N8O2

溶解度: DMSO ≥100mg/mL Water <1mg/mL Ethanol ≥5mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 955365-80-7

生物活性

 

MK-1775 is a potent and selective Wee1 kinase inhibitor with an IC50 of 5.2 nM. [1]

It abolishes cyclin-dependent kinase 1 (CDC2) activity by phosphorylation of the Tyr15 residue. It abrogates a DNA damage checkpoint (G2-phase), leading to apoptosis in combination with several DNA-damaging agents selectively in p53-deficient tumor cell lines. It is under clinical trial for advanced solid tumors. [2]

 

参考文献

New Insights into Checkpoint Kinase 1 in the DNA Damage Response Signaling Network Yun Dai and Steven Grant Clin Cancer Res 2010;16:376-383

MK-1775, a small molecule Wee1 inhibitor,enhances antitumor efficacy of various DNA-damaging agents, including 5-fluorouracil hiroshi hirai,Tsuyoshi Arai,et al. Cancer Biology & Therapy April 1, 2010;9:7, 514-522

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0 Comments

现货,MGCD-265,CAS号:875337-44-3,美国进口, 受体酪氨酸激酶(RTK) , c-Met ,c-Met 抑制剂,selleck,S1361

信号转导通路: 受体酪氨酸激酶(RTK) >> c-Met >> c-Met 抑制剂 >> MGCD-265http://selleck.cn/mgcd-265-S1361.html

技术数据:

分子量(MW): 517.60

化学式:

C26H20FN5O2S2

溶解度: DMSO ≥104mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 875337-44-3

生物活性

 

MGCD265 is a tyrosine kinase inhibitor that targets the MET, VEGFR-1, VEGFR-2, VEGFR-3, RON and TIE2 receptor tyrosine kinases, which appear to play key roles in tumour development and blood vessel formation (angiogenesis) and tumour survival. MGCD265 is currently in phase I single-agent clinical trials for solid tumour cancers and in phase II trials for solid tumours and NSCLC . [1]

 

参考文献

AMG 706, an Oral, Multikinase Inhibitor that Selectively Targets Vascular Endothelial Growth Factor, Platelet-Derived Growth Factor, and Kit Receptors, Potently Inhibits Angiogenesis and Induces Regression in Tumor Xenografts Angela Coxon, Charlie Starnes, et al. Cancer Res 2006;66:8715-8721

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0 Comments

现货,KW 2449 ,CAS号:1000669-72-6,美国进口, 血管生成(Angiogenesis), Flt , Flt 抑制剂,selleck,S2158

信号转导通路:  血管生成(Angiogenesis) >> Flt >> Flt 抑制剂 >> 

信号转导通路: 血管生成(Angiogenesis) >> Flt >> Flt 抑制剂 >> KW 2449http://www.selleck.cn/kw-2449-S2158.html

技术数据:

分子量(MW): 332.4

化学式:

C20H20N4O

 

溶解度: DMSO ≥67mg/mL Water <1mg/mL Ethanol ≥67mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1000669-72-6

生物活性

 

 

KW-2449, a multi-kinase inhibitor of FLT3(IC50 at 6.6pM), ABL(IC50 at 14pM), ABL-T315I and Aurora kinase, is under investigation to treat leukemia patients. KW-2449 potently and selectively inhibits the growth of leukemia cells harboring constitutively activated FLT3 kinase both in vitro and in vivo. In addition, it potently inhibitedABL-T315I, which is associated with IM resistance, with an IC50 value of 4 pM. On the other hand, KW-2449 had little effect on PDGFR, IGF- I R, EGFR, and various serine/threonine kinases even at a concentration of 1 uM. Among various serine/threonine kinases examined, KW-2449 inhibited Aurora A kinase with IC50 of 48 pMp and Aurora B kinase with the equivalent potenc. [1,2]

 

 

 

参考文献

KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation Yukimasa Shiotsu, Hitoshi Kiyoi,et al. Blood 2009;114: 1607-1617

A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response Keith W. Pratz, Jorge Cortes,et al. Blood 2009;113: 3938-3946

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0 Comments

现货,ZSTK474 , CAS号:475110-96-4,美国进口,PI3K / mTOR / AKT , PI3K, PI3K 抑制剂,selleck,S1072

信号转导通路:  PI3K / mTOR / AKT >> PI3K >> PI3K 抑制剂 >> 

信号转导通路: PI3K / mTOR / AKT >> PI3K >> PI3K 抑制剂 >> ZSTK474http://www.selleck.cn/zstk474-S1072.html

 

技术数据:

分子量(MW): 417.41

化学式:

C19H21F2N7O2

 

溶解度: DMSO ≥21mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 475110-96-4

生物活性

 

 

ZSTK474 is an inhibitor of PI3K γ (IC50 at 6 nM). This agent inhibits PI3K α and PI3K β with IC50 of 17 and 53 nM, respectively. ZSTK474 was identified from a chemical library of about 1500 triazine derivatives, and selected for their ability to block tumor cell growth. In preclinical studies ZSTK474 was orally administered to mice and displayed a strong anti-tumoral activity in xenograft models. Toxicity was reported to be moderate. [1]

 

 

 

参考文献

Targeting phosphoinositide 3-kinase—Moving towards therapy Romina Marone,Vladimir Cmiljanovic,et al. Biochimica et Biophysica Acta 2008;1784: 159–185

Antitumor Activity of ZSTK474, a New Phosphatidylinositol 3-Kinase Inhibitor Shin-ichi Yaguchi , Yasuhisa Fukui , et al. Journal of the National Cancer Institute April 19, 2006;98:545-556

客户反馈数据

 

We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.

 

 

 

 

Western blot analysis of Akt and p-Akt. 0-20μM ZSTK474 was added.

如果需要长期保存,请于零下二十度低温保存。

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0 Comments

现货,Elesclomol,CAS号:488832-69-5,美国进口,HDAC-HSP-Aurora , HSP90 , HSP90 抑制剂和化合物,selleck,S1052

信号转导通路: HDAC-HSP-Aurora >> HSP90 >> HSP90 抑制剂和化合物 >> Elesclomolhttp://selleck.cn/elesclomol-S1052.html

技术数据:

分子量(MW): 400.5

化学式:

C19H20N4O2S2

 

溶解度: DMSO ≥80mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: 99%

稳定性: at -20℃ 2 years

CAS号: 488832-69-5

生物活性

 

 

Elesclomol (STA-4783) is a small molecule that induces apoptosis via the mitochondrial apoptotic pathway in cancer cells by increasing oxidative stress, while having little or no effect on normal cells. It is a pro-apoptotic agent that demonstrates anti-tumor activity against a broad range of cancer cell types. It promotes apoptosis in Hs294T melanoma cells treated with 100 nmol/L for six hours by rapidly generating reactive oxygen species and inducing the transcription of Hsp70 and metallothionein.1 Stage III clinical trials to assess efficacy of elesclomol treatment in combination with paclitaxel2, 1 in patients with stage IV metastatic melanoma were suspended due to safety concerns.

 

 

 

参考文献

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0 Comments

现货,ON-01910 ,CAS号:1225497-78-8,美国进口,细胞周期(Cell Cycle / Checkpoint) , PLK , PLK 抑制剂,selleck,S1362

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> PLK >> PLK 抑制剂 >> ON-01910http://www.selleck.cn/on-01910-S1362.html

技术数据:

分子量(MW): 473.47

化学式:

C21H24NNaO8S

 

溶解度: DMSO ≥95mg/mL Water ≥95mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1225497-78-8

生物活性

 

 

ON-01910 is a non-ATP-competitive small molecule Plk1inhibitor with an IC50 of 9 nM. It induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis. This compound was not ATP-competitive, but competed for the substrate binding site of the enzyme. In vivo, this compound did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft nude mouse models. ON01910 showed strong synergy with several chemotherapeutic agents, often inducing complete regression of tumors. [1][2]

 

 

 

参考文献

ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent Kiranmai Gumireddy,M.V. Ramana Reddy,et al. CANCER CELL MARCH 2005;7:275-286

Targeted anti-mitotic therapies:can we improve on tubulin agents? Jeffrey R. Jackson,Denis R. Patrick,et al. CANCER FEBRUARY 2007;7:107-117

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0 Comments

现货,PIK-93 , CAS号:593960-11-3,美国进口,PI3K / mTOR / AKT , PI3K , PI3K 抑制剂,selleck,S1489

信号转导通路: PI3K / mTOR / AKT >> PI3K >> PI3K 抑制剂 >> PIK-93http://www.selleck.cn/pik-93-S1489.html

技术数据:

分子量(MW): 389.88

化学式:

C14H16ClN3O4S2

 

溶解度: DMSO ≥78mg/mL Water <1mg/mL Ethanol ≥2mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 593960-11-3

生物活性

 

 

PIK-93 is a PI4KIIIβ inhibitor (IC50 at 19 nM). PIK-93 is the first reported PI4-kinase inhibitor, which is able to inhibit PI4KIIIβ at low-nanomolar range. In addition, this compound also inhibits potently PI3Kγ in vitro (IC50 at 16 nM). This compound inhibits p110α, p110β, p110δwith IC50 of 0.039, 0.59, 0.12 µM. PIK-93 also displays the typical hydrogen bonding to the backbone amide of Val882, and additional ones to the backbone carbonyl of Val882 and between its sulphonamide and Asp964. [1]

 

 

 

参考文献

Targeting phosphoinositide 3-kinase—Moving towards therapy Romina Marone,Vladimir Cmiljanovic,et al. Biochimica et Biophysica Acta 2008;1784:159–185

客户反馈数据

After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PIK-93 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

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0 Comments

现货,SP600125 ,CAS号:129-56-6,美国进口,MAPK, JNK ,JNK 抑制剂和化合物,selleck,S1460

信号转导通路: MAPK >> JNK >> JNK 抑制剂和化合物 >> SP600125http://selleck.cn/sp600125-S1460.html

技术数据:

分子量(MW): 220.23

化学式:

C14H8N2O

 

溶解度: DMSO ≥44mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 129-56-6

生物活性

 

 

SP600125 is a JNK inhibitor (IC50=40 nM for JNK-1 and JNK-2 and 90 nM for JNK-3). This agent exhibits greater than 300-fold selectivity for JNK against related MAP kinases ERK1 and p38–2, and the serine threonine kinase PKA. [1]

SP600125 is a reversible ATP-competitive inhibitor. In cells, SP600125 dose dependently inhibited the phosphorylation of c-Jun, the expression of inflammatory genes COX-2, IL-2, IFN-γ, TNF-α, and prevented the activation and differentiation of primary human CD4 cell cultures. [1]

 

 

 

参考文献

SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase Brydon L. Bennett,Dennis T. Sasaki,et al. PNAS November 20, 2001;98:13681–13686

客户反馈数据

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0 Comments

现货,Semagacestat (LY450139),CAS号:425386-60-3,美国进口,神经信号通路(Neuronal Signaling) , Gamma-Secretase, Gamma-Secretase 抑制剂,S1594,selleck

信号转导通路: 神经信号通路(Neuronal Signaling) >> Gamma-Secretase >> Gamma-Secretase 抑制剂 >> Semagacestat (LY450139)http://www.selleck.cn/semagacestat-ly450139-S1594.html

技术数据:

分子量(MW): 361.44

化学式:

C19H27N3O4

 

溶解度: DMSO ≥72mg/mL Water <1mg/mL Ethanol ≥43mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 425386-60-3

生物活性

 

 

Semagacestat (LY450139) is a γ-secretase blocker with an IC50 of 15 nM.β-amyloid is a peptide of 39 to 43 amino acids. [1] The isoforms with 40 and 42 amino acids (Aβ40/42) are the main constituents of amyloid plaques in the brains of Alzheimer’s disease patients. β-amyloid is formed by proteolysis of APP. Research on laboratory rats suggest that the soluble form of this peptide is a causative agent in the development of Alzheimer’s. Semagacestat blocks the enzyme γ-secretase, which (along with β-secretase) is responsible for APP proteolysis. [2]

 

 

 

参考文献

Recent Advances in the Identification of γ-Secretase Inhibitors To Clinically Test the Aβ Oligomer Hypothesis of Alzheimer’s Disease Anthony F. Kreft, Robert Martone, et al. J. Med. Chem. 2009;52:6169–6188

http://en.wikipedia.org/wiki/Semagacestat http://en.wikipedia.org/wiki/Semagacestat ;

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0 Comments

现货,GSK461364 ,CAS号:929095-18-1,美国进口, 细胞周期(Cell Cycle / Checkpoint) , PLK, PLK 抑制剂,selleck,S2193

信号转导通路:  细胞周期(Cell Cycle / Checkpoint) >> PLK >> PLK 抑制剂 >> 

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> PLK >> PLK 抑制剂 >> GSK461364http://www.selleck.cn/gsk461364-S2193.html

技术数据:

分子量(MW): 543.6

化学式:

C27H28F3N5O2S

 

溶解度: DMSO ≥10mg/mL Water <1mg/mL Ethanol ≥63mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 929095-18-1

生物活性

 

 

GSK 461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM. GSK461364 is an ATP-competitive inhibitor of Plk1 and forms a rapidly reversible complex with Plk1. It has a 400-fold greater potency for Plk1 than for Plk2 and Plk3. It is > 100-fold selective with respect to PLk2, PLK3, and 48 other kinases tested. Treatment of 120 cell lines with GSK-461364 led to growth inhibition with an IC50 of < 100 nM in over 90% cases, with a net cytostatic response in about 40% and net cell death in 45% of cell lines tested. Interestingly, it caused dose-dependent mitotic arrest in Colo205 xenografts in vivo. [1][2]

 

 

 

参考文献

Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors Yoshiyuki Sato, Yu Onozaki, et al. Bioorg. Med. Chem. Lett 2009;19:4673–4678

Multifaceted polo-like kinases:drug targets and antitargets for cancer therapy Klaus Strebhardt Drug Discovery AuguST 2010;9:643-660

客户反馈数据

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现货,CUDC-101,CAS号:1012054-59-9,美国进口,HDAC-HSP-Aurora, HDAC , HDAC 抑制剂,selleck,S1194

信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂 >> CUDC-101http://www.selleck.cn/cudc-101-S1194.html

技术数据:

分子量(MW): 434.49

化学式:

C24H26N4O4

 

溶解度: DMSO ≥43mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: -20℃ 2 years

CAS号: 1012054-59-9

生物活性

 

 

CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 has novel structure incorporating HDAC inhibitory functionality into the pharmacophore of the EGFR and HER2 inhibitors. In most tumor cell lines tested, CUDC-101 exhibits efficient antiproliferative activity with greater potency than vorinostat (SAHA), erlotinib, lapatinib, and combinations of vorinostat/erlotinib and vorinostat/lapatinib. In vivo, CUDC-101 promotes tumor regression or inhibition in various cancer xenograft models including nonsmall cell lung cancer (NSCLC), liver, breast, head and neck, colon, and pancreatic cancers. [1][2]

 

 

 

参考文献

Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer Hai-Xiao Zhai, Jing Wang,et al. J. Med. Chem. 2010;3, 2000–2009

CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase,Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity Rudi Bao, Xu Tao, et al. Cancer Res 2010;70:3647-3656

客户反馈数据

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0 Comments

现货,SB 216763 ,CAS号:280744-09-4,美国进口, PI3K / mTOR / AKT, GSK-3,GSK-3 抑制剂和化合物,selleck,S1075

信号转导通路: PI3K / mTOR / AKT >> GSK-3 >> GSK-3 抑制剂和化合物 >> SB 216763http://selleck.cn/sb-216763-S1075.html

技术数据:

分子量(MW): 371.22

化学式:

C19H12N2O2Cl2

 

溶解度: DMSO ≥26mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 280744-09-4

生物活性

 

 

SB 216763 inhibited human GSK-3α with IC50s of 34 nM, when assayed in the presence of 0.01 mM ATP. This compounds inhibited GSK-3α in an ATP competitive manner. SB 216763 inhibited GSK-3α with Kis of 9nM.

In the presence of 0.1 mM ATP, 10 μM SB-216763 inhibited GSK-3β kinase activity by 96%. In contrast, this compounds exhibited little or no inhibition of the other 24 members of the kinase selectivity panel.

SB 216763 stimulated glycogen synthesis in the Chang human liver cell line with EC50s of 3.6 μM. The maximum effective concentrations of SB 216763 was 30 μM. [1]

 

 

 

参考文献

Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription Matthew P Coghlan,Ainsley A Culbert,et al. Chemistry & Biology 2000;7:793^803

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现货,Vicriviroc Malate ,微生物学(Microbiology), CCR5 , CCR5 抑制剂,selleck,目录号S2004

信号转导通路: 微生物学(Microbiology) >> CCR5 >> CCR5 抑制剂 >> Vicriviroc Malatehttp://www.selleck.cn/vicriviroc-malate-S2004.html

技术数据:

分子量(MW): 667.72

化学式:

C28H38F3N5O2.C4H6O5

 

溶解度: DMSO ≥134mg/mL Water ≥38mg/mL Ethanol ≥134mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 541503-81-5

生物活性

 

 

In order to determine if vicriviroc malate is a receptor agonist or antagonist, three functional assays were employed to measure the ability of the compound to block b-chemokine signaling in CCR5-expressing cells.A chemotaxis assay was first employed to determine the ability of vicriviroc malate to inhibit chemokine-mediated migration of a mouse Ba/F3 cell line stably expressing recombinant human CCR5. In this assay, vicriviroc malate showed equally potent inhibition of the chemotactic response to MIP-1 with IC50 values below 1 nM. The ability of vicriviroc malate to inhibit intracellular calcium release induced by receptor stimulation was also assessed. A assay utilized to demonstrate the ability of vicriviroc malate to inhibit CCR5 receptor signaling was a GTPS exchange assay. GTPS binding induced by RANTES. vicriviroc malate potently inhibited RANTES-induced signaling with mean IC50s of 4.2 nM. [1] Vicriviroc Malate is highly water-soluble and demonstrates oral bioavailability of >89% in rats and monkeys. The compound is modestly human plasma protein-bound (≈84%) and widely distributed in the extra vascular space.Absorption and exposure in humans are linear and doseproportional, with a terminal phase half-life >24 hours supportive of once daily dosing. Variability in absorption is modest (20–40%). [2] Vicriviroc Malate is NOT A p-glycoprotein Substrate In Vitro. [3]

 

 

 

参考文献

Discovery and Characterization of Vicriviroc (SCH 417690), a CCR5 Antagonist with Potent Activity against Human Immunodeficiency Virus Type 1 Julie M. Strizki,Cecile Tremblay,et al. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY Dec. 2005;49:4911–4919

Vicriviroc Is a Novel, Potent CCR5 Inhibitor With Outstanding Pharmaceutic, Pharmacokinetic and PharmaCodynamic (PK/PD) Properties Lisa Dunkle, Anther Keung,et al. Retrovirology 2005;2(Suppl 1):S12

Vicriviroc, A Novel CCR5 Inhibitor, is NOT A p-glycoprotein Substrate In Vitro Cheng Li,Anther Keung,et al. Retrovirology 2005;2(Suppl 1):P158

 

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,Tandutinib (MLN518) ,CAS号:387867-13-2,美国进口,血管生成(Angiogenesis) , Flt , Flt 抑制剂和化合物,selleck,S1043

信号转导通路: 血管生成(Angiogenesis) >> Flt >> Flt 抑制剂和化合物 >> Tandutinib (MLN518)http://selleck.cn/tandutinib-mln518-S1043.html

技术数据:

分子量(MW): 562.7

化学式:

C31H42N6O4

 

溶解度: DMSO ≥11mg/mL Water <1mg/mL Ethanol ≥19mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 387867-13-2

生物活性

 

 

The FMS-like tyrosine kinase 3 (FLT3) protein is a receptor tyrosine kinase that is expressed at high levels in 70-100% of cases of AML(Acute myeloid leukemia) and has been identified as potential target for molecular therapy. Internal tandem duplications (ITD) of the juxtamembrane domain in FLT3 occur regularly in de novo AML, resulting in constitutive activation of FLT3 tyrosine kinase activity. [1]

In cell-based assays tandutinib inhibited FLT3 ,PDGFR, and KIT with IC50 values of 95-122 ng/mL, but had no significant effect against a broad range of other kinases. In Ba/F3 cells expressing various FLT3-ITD mutants, tandutinib inhibited IL-3-independent growth and FLT3-ITD auto-phosphorylation with IC50 values of 6-17 ng/ml. Tandutinib also inhibited in vitro proliferation of human leukemia cell lines containing FLT3-ITD mutations with IC50 values of approximately 6 ng/mL. [2]

Tandutinib has a very limited spectrum of activity outside the type III receptor kinase family. Evaluation of tandutinib in rats, dogs, and monkeys showed it to be orally bioavailable, metabolically stable.

Phase I clinical results with tandutinib (MLN518) in patients with acute myelogenous leukemia or high-risk myelodysplastic syndrome: safety, pharmacokinetics, and pharmacodynamics.

 

 

 

参考文献

The FLT3 inhibitor tandutinib (formerly MLN518) has sequence-independent synergistic effects with cytarabine and daunorubicin Marcus M. Schittenhelm,Kerstin M. Kampa,et al. Cell Cycle 15 August 2009;8:16, 2621-263

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0 Comments

现货, TAK-875,CAS号:1000413-72-8,美国进口,内分泌/激素(E / H) , GPR , GPR 抑制剂,selleck,S2637

信号转导通路: 内分泌/激素(E / H) >> GPR >> GPR 抑制剂 >> TAK-875http://www.selleck.cn/tak-875-S2637.html

技术数据:

分子量(MW): 533.63

化学式:

C29H32O7S.1/2H2O

 

溶解度: DMSO ≥105mg/mL Water <1mg/mL Ethanol ≥11mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1000413-72-8

生物活性

 

 

TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with an EC50 of 0.072 μM. TAK-875 is a new agent applied in the treatment of type 2 diabetes. TAK-875 not only elevated the levels of intra-cellular inositol monophosphate as well as calcium contents in rat insulinoma INS-1 833/15 cells but also improved the tolerance of glucose and amplified insulin secretion when orally administered in tolerance test. However, TAK-875 didn’t increase the secretion of insulin and cause hypoglycemia when 30 mg/kg dosage of TAK-875 was given in fasted normal Sprague Dawley rats. Conversely, TAK-875 with a dosage of 10 mg/kg (p.o.) not only significantly improved plasma insulin levels but also decreased fasting hyperglycemia in male Zucker diabetic fatty rats. [1][2]

 

 

 

参考文献

TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. Tsujihata Y et al. J Pharmacol Exp Ther. 2011 Jul 13;

http://clinicaltrials.gov/ct2/show/NCT00949091 http://clinicaltrials.gov/ct2/show/NCT00949091 ;

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现货,BMS-790052,CAS号1214735-16-6,美国进口,蛋白酶体(Proteases) , HCV Protease, HCV Protease 抑制剂,selleck,S1482

信号转导通路: 蛋白酶体(Proteases) >> HCV Protease >> HCV Protease 抑制剂 >> BMS-790052http://www.selleck.cn/bms-790052-S1482.html

技术数据:

分子量(MW): 738.88

化学式:

C40H50N8O6

 

溶解度: DMSO ≥148mg/mL Water <1mg/mL Ethanol ≥148mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1214735-16-6

生物活性

 

 

Daclatasvir (BMS-790052) is a first-in-class, highly-selective oral HCV NS5A inhibitor. NS5A is an essential component for hepatitis C virus (HCV) replication complex. Daclatasvir (BMS-790052) has broad genotype coverage and exhibits picomolar in vitro potency against genotypes 1a (EC50 50pm) and 1b (EC50 9pm). Daclatasvir (BMS-790052) produces a robust decline in HCV RNA (-3.6 logs after 48 hours from a single 100 mg) dosefollowing a single dose in patients chronically infected with HCV genotype 1. [1,2]

 

 

 

参考文献

Resistance Analysis of the Hepatitis C Virus NS5A Inhibitor BMS-790052 in an In Vitro Replicon System Robert A. Fridell,Dike Qiu,et al. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY Sept. 2010;54:3641–3650

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect Min Gao,Richard E. Nettles,et al. Nature 6 May 2010;465:96-100

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0 Comments

现货,BMS-790052,CAS号1214735-16-6,美国进口,蛋白酶体(Proteases) , HCV Protease, HCV Protease 抑制剂,selleck,S1482

信号转导通路: 蛋白酶体(Proteases) >> HCV Protease >> HCV Protease 抑制剂 >> BMS-790052http://www.selleck.cn/bms-790052-S1482.html

技术数据:

分子量(MW): 738.88

化学式:

C40H50N8O6

 

溶解度: DMSO ≥148mg/mL Water <1mg/mL Ethanol ≥148mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1214735-16-6

生物活性

 

 

Daclatasvir (BMS-790052) is a first-in-class, highly-selective oral HCV NS5A inhibitor. NS5A is an essential component for hepatitis C virus (HCV) replication complex. Daclatasvir (BMS-790052) has broad genotype coverage and exhibits picomolar in vitro potency against genotypes 1a (EC50 50pm) and 1b (EC50 9pm). Daclatasvir (BMS-790052) produces a robust decline in HCV RNA (-3.6 logs after 48 hours from a single 100 mg) dosefollowing a single dose in patients chronically infected with HCV genotype 1. [1,2]

 

 

 

参考文献

Resistance Analysis of the Hepatitis C Virus NS5A Inhibitor BMS-790052 in an In Vitro Replicon System Robert A. Fridell,Dike Qiu,et al. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY Sept. 2010;54:3641–3650

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect Min Gao,Richard E. Nettles,et al. Nature 6 May 2010;465:96-100

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现货,Regorafenib (BAY 73-4506) ,CAS号:755037-03-7,受体酪氨酸激酶(RTK) , c-Kit , c-Kit 抑制,selleck,S1178

信号转导通路: 受体酪氨酸激酶(RTK) >> c-Kit >> c-Kit 抑制剂 >> Regorafenib (BAY 73-4506)http://www.selleck.cn/bay-73-4506-S1178.html

技术数据:

分子量(MW): 482.82

化学式:

C21H15ClF4N4O3

 

溶解度: DMSO ≥97mg/mL Water <1mg/mL Ethanol ≥8mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 755037-03-7

生物活性

 

 

Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature. Regorafenib (BAY 73-4506) binds to and inhibits VEGFR-2 and -3, and tumor cell signaling kinases (RET, KIT, PDGFR, and Raf), which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. Regorafenib (BAY 73-4506) shows potent, oral activity in a wide variety of preclinical xenograft models. [1]

 

 

 

参考文献

Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity Scott M. Wilhelm,Jacques Dumas,et al. International Journal of Cancer 2011;129:245-255

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0 Comments

现货,JNJ-26481585,CAS号:875320-29-9,美国进口, HDAC-HSP-Aurora,HDAC ,HDAC 抑制剂和化合物,selleck,S1096

信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂和化合物 >> JNJ-26481585http://selleck.cn/jnj-26481585-S1096.html

技术数据:

分子量(MW): 394.476

化学式:

C21H26N6O2

 

溶解度: DMSO ≥79mg/mL Water ≥50mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 875320-29-9

生物活性

 

 

JNJ-26481585 is an orally bioavailable, second-generation, hydroxamic acid-based HDAC inhibitor with an IC50 of 2.43 nM for 5T33MMvt cells. JNJ-26481585 has potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. [1] In vitro, JNJ-26481585 induced caspase cascade activation and upregulation of p21, resulting in apoptosis and cell cycle arrest in the myeloma cells at low nanomolar concentrations. When the 5T2MM-bearing mice were treated with JNJ-26481585, there were a reduction of the tumor load and a significant decrease in angiogenesis. [2]

 

 

 

 

 

参考文献

Bortezomib Alone or in Combination with the Histone Deacetylase Inhibitor JNJ-26481585: Effect on Myeloma Bone Disease in the 5T2MM Murine Model of Myeloma Miguel Lemaire, Janine Arts, et al. Cancer Res 2009;69:5307-5311

The effects of JNJ-26481585, a novel hydroxamate-based histone deacetylase inhibitor,on the development of multiple myeloma in the 5T2MM and 5T33MM murine models S Deleu,M Lemaire,et al. Leukemia 2009;23:1894–1903

 

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现货,E7080 ,CAS号:417716-92-8,美国进口, 受体酪氨酸激酶(RTK) , VEGFR , VEGFR 抑制剂和化合物,selleck,S1164

信号转导通路: 受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR 抑制剂和化合物 >> E7080http://selleck.cn/e7080-S1164.html

技术数据:

分子量(MW): 426.85

化学式:

C21H19ClN4O4

 

溶解度: DMSO ≥16mg/mL Water <1mg/mL Ethanol ≥1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 417716-92-8

生物活性

 

 

E7080 is the most potent dual inhibitor of VEGF-R3 tyrosine kinase (IC50=5.2 nM) as well as VEGF-R2 tyrosine kinase (IC50=4.0 nM) among those small-molecule inhibitors of VEGF-R kinases, such as sunitinib, sorafenib, and CEP-7055. It has been evaluated in vitro (pre-clinical) for anti-cancer effects. E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of angiogenesis and lymphangiogenesis. [2,3]

It has had promising results from a phase I clinical trial in 2006 and is being tested in several Phase I and II trials as of October 2009, for example against hepatocellular carcinoma and non-small cell lung carcinoma. [1]

 

 

 

参考文献

Tyrosine Kinase Inhibitor, Suppresses the − E7080, a Multi Progression of Malignant Pleural Mesothelioma with Different Proangiogenic Cytokine Production Profiles Seiji Yano, Van The Trung, et al. Clin Cancer Res 2009;15:7229-7237

Multi-Kinase Inhibitor E7080 Suppresses Lymph Node and Lung Metastases of Human Mammary Breast Tumor MDA-MB-231 via Inhibition of Vascular Endothelial Growth Factor-Receptor (VEGF-R) 2 and VEGF-R3 Kinase Yasuhiro Funahashi, Toshimitsu Uenaka, et al. Clin Cancer Res 2008;14:5459-5465

E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition Junji Matsui,Yuji Yamamoto,et al. Int. J. Cancer 2008;122:664–671

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现货,Elvitegravir (GS-9137) ,CAS号:697761-98-1,美国进口, 微生物学(Microbiology) , Integrase , Integrase 抑制剂,selleck,S2001

信号转导通路: 微生物学(Microbiology) >> Integrase >> Integrase 抑制剂 >> Elvitegravir (GS-9137)http://selleck.cn/elvitegravir-S2001.html

技术数据:

分子量(MW): 447.88

化学式:

C23H23ClFNO5

 

溶解度: DMSO ≥90mg/mL Water <1mg/mL Ethanol ≥90mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 697761-98-1

生物活性

 

 

Elvitegravir (GS-9137) is a human immunodeficiency virus integrase inhibitor with EC50 of 0.7, 2.8 and 1.4 for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD. Elvitegravir (GS-9137) plays an essential role in the integration of proviral DNA into the host genome. Interestingly, elvitegravir (GS-9137) also showed antiviral activity against murine leukemia virus (MLV) and simian immunodeficiency virus (SIV). EVG inhibited the integration of the HIV-based vector used as a positive control for the luciferase assay (EC50 values of 0.8 nM), as observed in the MAGI assay with HIV-1IIIB. Elvitegravir (GS-9137) suppressed the replication of MLV infection (EC50 values of 5.8 nM) as well as that of the primate retrovirus SIV (0.5 nM), indicating that IN inhibitors have antiviral activity against a broad range of retroviruses. [1][2][3]

 

 

 

参考文献

Molecular mechanisms in retrovirus DNA integration Ernest Asante-Appiah, Anna Marie Skalka Antiviral Research 1997;36 :139–156

A quantitative assay for HIV DNA integration in vivo SCOTT L. BUTLER, MARK S.T. HANSEN,et al. NATURE MEDICINE MAY 2001;7:631-634

Broad Antiretroviral Activity and Resistance Profile of the Novel Human Immunodeficiency Virus Integrase Inhibitor Elvitegravir (JTK-303/GS-9137) Kazuya Shimura,Eiichi Kodama,et al. JOURNAL OF VIROLOGY Jan. 2008;82:764–774

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现货,17-DMAG (Alvespimycin),CAS号:467214-21-7,美国进口,HDAC-HSP-Aurora, HSP90,HSP90 抑制剂和化合物

信号转导通路: HDAC-HSP-Aurora >> HSP90 >> HSP90 抑制剂 >> 17-DMAG HCl (Alvespimycin)http://www.selleck.cn/17-dmag-alvespimycin-S1142.html

技术数据:

分子量(MW): 653.21

化学式:

C32H48N4O8•HCl

 

溶解度: DMSO ≥131mg/mL Water ≥3mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 467214-21-7

生物活性

 

 

17-DMAG HCl (Alvespimycin), a watersoluble geldanamycin analog belonging to the class of benzoquinones, is a selective Hsp90 inhibitor. 17-DMAG HCl binds to the N-terminal domain ATP binding site of Hsp90, inhibiting Hsp90 chaperone activity. 17-DMAG HCl demonstrates greater potency and water solubility than other geldanamycin analogs such as 17-AAG (mean GI50 values are 53 and 123 nM for 17-DMAG HCl and 17-AAG respectively), while demonstrating anti-tumor activity and offering excellent oral bioavailability.[1]

 

 

 

 

 

参考文献

Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models Victoria Smith,Edward A. Sausville,et al. Cancer Chemother Pharmacol 2005;56: 126–137

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现货,NVP-ADW742,CAS号:475488-23-4,美国进口, 受体酪氨酸激酶(RTK) , IGF-1R , IGF-1R 抑制剂和化合物,S1088,selleck,

信号转导通路: 受体酪氨酸激酶(RTK) >> IGF-1R >> IGF-1R 抑制剂 >> NVP-ADW742http://selleck.cn/nvp-adw742-S1088.html

技术数据:

分子量(MW): 453.58

化学式:

C28H31N5O

 

溶解度: DMSO ≥14mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 475488-23-4

生物活性

 

 

NVP-ADW742 is an ATP-competitive inhibitor that inhibits IGF-1R autophosphorylation with a cellular IC50 of 0.1 to 0.2μmol/L, which is 16-fold lower than that of the insulin receptor[1] . NVP-ADW742 also enhances the sensitivity of SCLC to etoposide and carboplatin, which are commonly used in the treatment of SCLC[2] .

 

 

 

参考文献

The Insulin-Like Growth Factor-I Receptor Kinase Inhibitor,NVP-ADW742, Sensitizes Small Cell Lung Cancer Cell Lines to the Effects of Chemotherapy Julie Litz, Elisabeth Buchdunger, et al. Clin Cancer Res 2005;11:1563-1571

The insulin-like growth factor-I (IGF-I) receptor kinase inhibitor NVP-ADW742, in combination with STI571,delineates a spectrum of dependence of small cell lung cancer on IGF-I and stem cell factor signaling Julie Litz, Elisabeth Buchdunger, et al Mol Cancer Ther 2004;3:527-536

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现货,AT7867 ,CAS号:857531-00-1,美国进口, PI3K / mTOR / AKT , AKT ,AKT 抑制剂和化合物,selleck,S1558

信号转导通路: PI3K / mTOR / AKT >> AKT >> AKT 抑制剂 >> AT7867http://www.selleck.cn/at7867-S1558.html

技术数据:

分子量(MW): 337.85

化学式:

C20H20ClN3

 

溶解度: DMSO ≥68mg/mL Water <1mg/mL Ethanol ≥5mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 857531-00-1

生物活性

 

 

AT7867 is a potent and oral AKT and p70 S6 kinase inhibitor with an IC50 of 17 nM.

Induction of apoptosis was detected by multiple methods in tumor cells following AT7867 treatment. Administration of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) to athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model caused inhibition of phosphorylation of downstream substrates of both AKT and p70S6K and induction of apoptosis, confirming the observations made in vitro. These doses of AT7867 also resulted in inhibition of human tumor growth in PTEN-deficient xenograft models. [1]

 

 

 

 

参考文献

AT7867 Is a Potent and Oral Inhibitor of AKT and p70 S6 Kinase That Induces Pharmacodynamic Changes and Inhibits Human Tumor Xenograft Growth Lisa-Jane K. Hunter, Timothy A. Yap, et al. Mol Cancer Ther 2010;9:1100-1110

 

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现货,Motesanib Diphosphate (AMG-706) ,CAS号:857876-30-3,美国进口,受体酪氨酸激酶(RTK) , VEGFR , VEGFR 抑制剂,selleck,S1032

信号转导通路: 受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR 抑制剂 >> Motesanib Diphosphate (AMG-706)http://selleck.cn/motesanib-diphosphate-S1032.html

技术数据:

分子量(MW): 569.44

化学式:

C22H23N5O.2H3PO4

 

溶解度: DMSO ≥114mg/mL Water ≥114mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 857876-30-3

生物活性

 

 

Motesanib (AMG-706) is an orally bioavailable diphosphate salt of a multiple receptor tyrosine kinase inhibitor with potential antineoplastic activity[1]. This reagent selectively targets and inhibits VEGFR1/2/3(IC50: 2 nM /3 nM /6 nM), PDGFR (84nM), kit (8nM), and Ret (59nM)receptors, thereby inhibiting angiogenesis and cellular proliferation. Oral administration of AMG 706 potently inhibited VEGF-induced angiogenesis in the rat corneal model and induced regression of established A431 xenografts [1] .This compound also performed antitumor activity in breast cancer xenografts and was currently being studied in clinical trials for the treatment of thyroid cancer and other advanced solid tumors[2,3,4]

 

 

 

 

参考文献

AMG 706, an Oral, Multikinase Inhibitor that Selectively Targets Vascular Endothelial Growth Factor,Platelet-Derived Growth Factor, and Kit Receptors, Potently Inhibits Angiogenesis and Induces Regression in Tumor Xenografts Angela Coxon, Charlie Starnes, et al. Cancer Res 2006;66:8715-8721

Broad Antitumor Activity in Breast Cancer Xenografts by Motesanib, a Highly Selective, Oral Inhibitor of Vascular Endothelial Growth Factor, Platelet-Derived Growth Factor,and Kit Receptors Tammy Bush, Douglas Saffran, et al. Clin Cancer Res 2009;15:110-118

Motesanib Diphosphate in Progressive Differentiated Thyroid Cancer Steven I. Sherman, Lori J. Wirth,et al. N Engl J Med 2008;359:31-42

Safety, Pharmacokinetics, and Efficacy of AMG 706, an Oral Multikinase Inhibitor, in PatientsWith Advanced Solid Tumors Lee S. Rosen, Razelle Kurzrock,et al. J Clin Oncol 2007;25:2369-2376.

 

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现货,WP1130,CAS号:856243-80-6,美国进口,受体酪氨酸激酶(RTK) ,Bcr-Abl , Bcr-Abl 抑制剂 ,selleck,目录号S2243

信号转导通路: 受体酪氨酸激酶(RTK) >> Bcr-Abl >> Bcr-Abl 抑制剂 >> WP1130http://selleck.cn/wp1130-S2243.html

技术数据:

分子量(MW): 384.27

化学式:

C19H18BrN3O

 

溶解度: DMSO ≥77mg/mL Water <1mg/mL Ethanol ≥77mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 856243-80-6

生物活性

 

 

WP1130 is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells. WP1130 acts as a partly selective deubiquitinases (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function. WP1130-mediated inhibition of tumor-activated DUBs results in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53. WP1130 specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. WP1130 was more effective in reducing leukemic versus normal hematopoietic colony formation and strongly inhibited colony formation of cells derived from patients with T315I mutant Bcr/Abl-expressing CML in blast crisis. Collectively, WP1130 reduces wild-type and T315I mutant Bcr/Abl protein levels in CML cells through a unique mechanism and may be useful in treating CML. [1][2]

 

 

 

参考文献

Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells Geoffrey A. Bartholomeusz, Moshe Talpaz,et al. Blood 2007;109: 3470-3478

Deubiquitinase Inhibition by Small-Molecule WP1130 Triggers Aggresome Formation and Tumor Cell Apoptosis Luke F. Peterson, Dexing Fang, et al. Cancer Res 2010;70:9265-9276

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0 Comments

现货,MLN8054 ,CAS号:869363-13-3,美国进口,HDAC-HSP-Aurora , Aurora Kinase , Aurora Kinase 抑制剂,selleck,S1100

信号转导通路: HDAC-HSP-Aurora >> Aurora Kinase >> Aurora Kinase 抑制剂 >> MLN8054http://www.selleck.cn/mln8054-S1100.html

技术数据:

分子量(MW): 476.86

化学式:

C25H15ClF2N4O2

 

溶解度: DMSO ≥95mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >97%

稳定性: at -20℃ 2 years

CAS号: 869363-13-3

生物活性

 

 

MLN8054 is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity[1] .

MLN8054 inhibits recombinant Aurora A kinase activity in vitro and is selective for Aurora A (IC50 = 0.004 μM)over the family member Aurora B (IC50 = 0.172 μM)in cultured cells[2]. MLN8054 treatment results in G2/M accumulation and spindle defects and inhibits proliferation in multiple cultured human tumor cells lines (IC50 0.11-0.86μM) [2] . Growth of human tumor xenografts in nude mice was dramatically inhibited after oral administration of MLN8054 at well tolerated doses[2] .

 

 

 

参考文献

MLN8054, a Small-Molecule Inhibitor of Aurora A, Causes Spindle Pole and Chromosome Congression Defects Leading to Aneuploidy Kara Hoar,Arijit Chakravarty,et al. MOL.CELL.BIOL. June 2007;27:4513–4525

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase Mark G. Manfredi,Jeffrey A. Ecsedy,et al. PNAS March 6, 2007;104:4106–4111

 

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现货,MLN9708,CAS号:1201902-80-8,美国进口,蛋白酶体(Proteases), Proteasome, Proteasome 抑制剂,selleck,S2181

信号转导通路: 蛋白酶体(Proteases) >> Proteasome >> Proteasome 抑制剂 >> MLN9708http://www.selleck.cn/mln9708-S2181.html

技术数据:

分子量(MW): 517.12

化学式:

C20H23BCl2N2O9

 

溶解度: DMSO ≥103mg/mL Water <1mg/mL Ethanol ≥5mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1201902-80-8

生物活性

 

 

MLN9708 is an orally bioavailable second generation proteasome inhibitor with potential antineoplastic activity. MLN9708 rapidly hydrolyzes to MLN2238, the biologically active form. It has a shorter proteasome dissociation half-life and improved pharmacokinetics, pharmacodynamics, and antitumor activity compared with bortezomib. It has a larger blood volume distribution at steady state, and analysis of 20S proteasome inhibition and markers of the unfolded protein response confirmed that MLN9708 has greater pharmacodynamic effects in tissues than bortezomib. MLN9708 showed activity in both solid tumor and hematologic preclinical xenograft models, and we found a correlation between greater pharmacodynamic responses and improved antitumor activity. [1][2][3]

 

 

 

参考文献

Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer Edmund C. Lee, Yueying Cao, et al. Cancer Res 2010;70:1970-1980

http://www.cancer.gov/drugdictionary/?CdrID=635527 http://www.cancer.gov/drugdictionary/?CdrID=635527 ;

http://ash.confex.com/ash/2010/webprogram/Paper31616.html http://ash.confex.com/ash/2010/webprogram/Paper31616.html ;

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现货,MP-470 ,CAS号:850879-09-3,美国进口, 受体酪氨酸激酶(RTK) ,c-Met ,c-Met 抑制剂,selleck,S1244

信号转导通路: 受体酪氨酸激酶(RTK) >> c-Met >> c-Met 抑制剂 >> MP-470http://www.selleck.cn/mp-470-S1244.html

技术数据:

分子量(MW): 447.51

化学式:

C23H21N5O3S

 

溶解度: DMSO ≥32mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 850879-09-3

生物活性

 

 

MP-470 is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM. MP-470(MP 470, MP470) reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. Cells pretreated with MP-470 had more ds DNA damage than cells treated with radiation alone. Mechanistically, MP-470 was shown to inhibit dsDNA break repair and increase apoptosis. [1][2] In a study, the cytotoxicity of MP-470 was evaluated on prostate cancer cell lines (LNCaP, PC-3 and DU-145). MP-470(MP 470, MP470) was effective on LNCaP and PC-3 cells with IC50 of ~4 μM and 8 μM, respectively. [3]

 

 

 

参考文献

The c-Met receptor tyrosine kinase inhibitor MP470 radiosensitizes glioblastoma cells James W Welsh,Daruka Mahadevan,et al. Radiation Oncology 2009;4:69

MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer Wenqing Qi,Larry S Cooke,et al. BMC Cancer 2009; 9:142

客户反馈数据

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0 Comments

现货,AZD6482 ,CAS号:1173900-33-8,美国进口,PI3K / mTOR / AKT, PI3K , PI3K 抑制剂,selleck,S1462

 

信号转导通路: PI3K / mTOR / AKT >> PI3K >> PI3K 抑制剂 >> AZD6482http://www.selleck.cn/azd6482-S1462.html

技术数据:

分子量(MW): 408.45

化学式:

C22H24N4O4

 

溶解度: DMSO ≥82mg/mL Water <1mg/mL Ethanol ≥28mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1173900-33-8

生物活性

 

 

AZD6482 is a PI3Kβ inhibitor (IC50=0.021μM) used in antithrombotic therapy. This agent targets a process that is critical to pathological thrombus formation without interfering with normal haemostasis, which avoids the drawbacks of the existing anti-thrombotic therapy. This agent inhibits PI3Kβ/α/γ/δwith IC50 of 0.021, 1.4, 1.2, 0.08μM, respectively. It washed platelet aggregation with concentration at 6 nM.

 

 

 

参考文献

客户反馈数据

如果需要长期保存,请于零下二十度低温保存。

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特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20 ° C ,抗体及蛋白等产品建议-60℃。抑制剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。

 

 

 

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0 Comments

现货,ITF2357 (Givinostat) ,CAS号: 732302-99-7,美国进口, HDAC-HSP-Aurora , HDAC , HDAC 抑制剂,selleck,S2170

信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂 >> ITF2357 (Givinostat)http://www.selleck.cn/itf2357-givinostat-S2170.html

技术数据:

分子量(MW): 475.97

化学式:

C24H27N3O4.HCl.H2O

 

溶解度: DMSO ≥95mg/mL Water ≥2mg/mL Ethanol ≥9mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 732302-99-7

生物活性

 

 

ITF2357 (Givinostat) is a noverl HDAC inhibitor with IC50 of 10, 7.5 and 16 nM for maize HDAC preparations HD2, HD-1B and HD-1A, respectively. ITF2357 (Givinostat) inhibits both class I and class II HDAC. ITF2357 (Givinostat) induces apoptosis of MM and acute myelogenous leukemia (AML) cells and this apoptosis takes place following induction of p21 and down-modulation of Bcl-2 and Mcl-1 proteins. When tested on normal cells, ITF2357 (Givinostat) inhibits the production of pro-inflammatory cytokines such as IL-1, IL-6, tumor necrosis factor (TNF)-α, and interferon (IFN)-γ by peripheral blood mononuclear cells and of IL-6 and vascular endothelium growth factor (VEGF) by mesenchymal stromal cells. ITF2357 (Givinostat) reduced the total intracellular IL-1α synthesis in freshly obtained PBMCs with 50% inhibition at concentrations below 25 nM. [1][2][3][4]

 

 

 

参考文献

The oral histone deacetylase inhibitor ITF2357 reduces cytokines and protects islet beta-cells in vivo and in vitro Eli C. Lewis,Lykke Blaabjerg,et al. Molecular Medicine ;Lewis,. et al page 1

Pleiotropic anti-myeloma activity of ITF2357: inhibition of interleukin-6 receptor signaling and repression of miR-19a and miR-19b Katia Todoerti,Valentina Barbui,et al. Haematologica 2010;95:260-269

Histone deacetylase inhibitor ITF2357 is neuroprotective, improves functional recovery, and induces glial apoptosis following experimental traumatic brain injury Naama A. Shein,Nikolaos Grigoriadis,et al. The FASEB Journal December 2009;23:4266-4275

http://en.wikipedia.org/wiki/Givinostat http://en.wikipedia.org/wiki/Givinostat ;

 

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0 Comments

现货,R935788 (Fostamatinib disodium, R788),CAS号:1025687-58-4,美国进口,受体酪氨酸激酶(RTK) ,Syk 抑制剂,selleck,目录号: S2206

信号转导通路: 受体酪氨酸激酶(RTK) >> Syk >> Syk 抑制剂 >> R935788 (Fostamatinib disodium, R788)http://selleck.cn/R935788-Fostamatinib-disodium-S2206.html

技术数据:

分子量(MW): 624.42

化学式:

C23H24FN6O9P.2Na

 

溶解度: DMSO <1mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1025687-58-4

生物活性

 

 

R935788 (Fostamatinib disodium, R788) is a selective Syk inhibitor with an IC50 of 41 nM.R935788 (Fostamatinib disodium) has shown clinical activity in heavily pre-treated NHL and CLL patients, exhibits inhibitory activity against SYK but also inhibits a broad spectrum of other kinase targets. In addition to blocking FcγR-mediated events,R935788 (Fostamatinib disodium, R788) also blocked BCR-mediated Ag presentation, thus broadly interrupting the humoral contributions to T cell-driven autoimmunity. Indeed, oral administration of R935788 (Fostamatinib disodium, R788) significantly delayed spontaneous diabetes onset in NOD mice and successfully delayed progression of early-established diabetes even when treatment was initiated after the development of glucose intolerance. At the DC level, R788 treatment was associated with reduced insulin-specific CD8 priming and decreased DC numbers. At the B cell level, R935788 (Fostamatinib disodium, R788) reduced total B cell numbers and total Ig concentrations. Interestingly, R935788 (Fostamatinib disodium, R788) increased the number of IL-10–producing B cells, thus inducing a tolerogenic B cell population with immunomodulatory activity. Taken together, Syk in APCs is an attractive target in T cell-mediated autoimmune diseases such as type 1 diabetes. [1][2][3][4]

 

 

 

参考文献

Fostamatinib, a Syk-kinase inhibitor, does not affect methotrexate pharmacokinetics in patients with rheumatoid arthritis. Baluom M et al. J Clin Pharmacol. 2011 Jan 5.;

The Syk kinase as a therapeutic target in leukemia and lymphoma. Efremov DG et al. Expert Opin Investig Drugs. ;

The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Eμ- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. Suljagic M et al. Blood. 2010 Dec 2.;116(23):4894-905.

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现货,KU-0063794,CAS号:938440-64-3,美国进口,PI3K / mTOR / AKT,mTOR,mTOR 抑制剂和化合物,selleck,目录号:S1226

信号转导通路: PI3K / mTOR / AKT >> mTOR >> mTOR 抑制剂和化合物 >> KU-0063794http://www.selleck.cn/ku-0063794-S1226.html

技术数据:

分子量(MW): 465.54

化学式:

C25H31N5O4

 

溶解度: DMSO ≥11mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 938440-64-3

生物活性

 

 

Ku-0063794 is a specific inhibitor of mTOR, which inhibits both mTORC1 and mTORC2 with an IC50 of approximately 10 nM, but does not suppress the activity of 76 other protein kinases or seven lipid kinases, including Class 1 PI3Ks at 1000-fold higher concentrations. Ku-0063794 is cell permeant, suppresses activation and hydrophobic motif phosphorylation of Akt, S6K and SGK. Ku-0063794 also suppressed cell growth and induced a G1-cell-cycle arrest. Ku-0063794 is a prototype of mTOR inhibitor AZD8055 currently in Phase I/II trial in Advance Solid Tumors, Lymphoma and Endometrial Carcinoma. [1]

 

 

 

参考文献

Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR) Juan M. GARCIA-MARTINEZ,Jennifer MORAN,et al. Biochem. J 2009;421:29–42

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0 Comments

现货,KU-60019 ,CAS号:925701-49-1,美国进口,PI3K / mTOR / AKT , ATM , ATM 抑制剂,selleck,S1570

信号转导通路: PI3K / mTOR / AKT >> ATM >> ATM 抑制剂 >> KU-60019http://www.selleck.cn/ku-60019-S1570.html

技术数据:

分子量(MW): 547.67

化学式:

C30H33N3O5S

 

溶解度: DMSO ≥48mg/mL Water <1mg/mL Ethanol ≥21mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 925701-49-1

生物活性

 

 

KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. As expected, KU-60019 is a highly effective radiosensitizer of human glioma cells. A-T fibroblasts were not radiosensitized by KU-60019, strongly suggesting that the ATM kinase is specifically targeted. Furthermore, KU-60019 reduced basal S473 AKT phosphorylation, suggesting that the ATM kinase might regulate a protein phosphatase acting on AKT. In line with this finding, the effect of KU-60019 on AKT phosphorylation was countered by low levels of okadaic acid, a phosphatase inhibitor, and A-T cells were impaired in S473 AKT phosphorylation in response to radiation and insulin and unresponsive to KU-60019. [1]

 

 

 

参考文献

Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling,and inhibits migration and invasion Sarah E. Golding,Elizabeth Rosenberg,et al. Mol Cancer Ther 2009 October;8(10): 2894–2902

 

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现货,AS703026,CAS号:1236699-92-5,美国进口, MAPK ,MEK , MEK 抑制剂和化合物,selleck,S1475

信号转导通路: MAPK >> MEK >> MEK 抑制剂 >> AS703026http://www.selleck.cn/as703026-S1475.html

技术数据:

分子量(MW): 431.20

化学式: C15H15FIN3O3

溶解度: DMSO ≥86mg/mL Water <1mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1236699-92-5

 

生物活性

 

AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor, in human multiple myeloma (MM). AS703026 inhibited growth and survival of MM cells (cell IC50 ranging from 0.005 to 2 μM) and cytokine-induced osteoclast differentiation more potently (9- to 10-fold) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression.

Importantly, AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. [1]

 

参考文献

Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Kim K, et al. Br J Haematol. 2010 May;149(4):537-49.

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现货,MC1568,CAS号: 852475-26-4 ,美国进口,HDAC-HSP-Aurora , HDAC ,HDAC 抑制剂和化合物,slleck,目录号S1484

信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂 >> MC1568http://www.dxy.cn/redirect?url=http://selleck.cn/mc1568-S1484.html

技术数据:

分子量(MW): 314.31

化学式:

C17H15FN2O3

溶解度: DMSO ≥13mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 852475-26-4

生物活性

 

MC1568 is a potent selective class II (IIa) histone deacetylas (HDAC II) inhibitor (IC50 of a maize deacetylase HD2 at 22.0 µM). MC1568 had no or a weak effect on the class I HDACs. MC1568 shows no inhibitory activity against HDAC1 but was able to inhibit HDAC4. [1]

 

参考文献

Specific activity of class II histone deacetylases in human breast cancer cells Vanessa Duong,Caroline Bret,et al. Mol Cancer Res 2008 December;6(12): 1908–1919

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现货,Danoprevir,CAS号:850876-88-9,美国进口,蛋白酶体(Proteases) ,Proteasome , Proteasome 抑制剂

信号转导通路: 蛋白酶体(Proteases) >> Proteasome >> Proteasome 抑制剂 >> Danoprevirhttp://www.dxy.cn/redirect?url=http://www.selleck.cn/danoprevir-S1183.html

技术数据:

分子量(MW): 717.85

化学式:

C35H48FN5O8S

 

溶解度: DMSO ≥144mg/mL Water <1mg/mL Ethanol ≥144mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 850876-88-9

生物活性

 

 

Danoprevir is a highly potent, orally absorbed inhibitor of the NS3/4A protease for treating chronic HCV infections. This agent is currently in Phase 2b study. [1] In biochemical assays using HCV NS3/4A protease domains derived from genotypes 1b, 1a, 2, or 3, the EC50 value of Danoprevir is <300 pM, 400 pM, 400 pM and 12.4 nM, respectively. Its EC50 value against full-length genotype-1b protease is 900 pM. Danoprevir retains subnanomolar to low-nanomolar potency against the NS3/4A variants at positions A156 and D168 that confer resistance to other experimental NS3/4A inhibitors.[1]Danoprevir is 97.9% bound by human plasma protein, and its replicon potency is shifted modestly by human serum. Danoprevir does not inhibit a panel of selected serine proteases, a broader ligand panel, or hERG ion channel. Its CC50 value is >50 mM. ITMN-191 does not inhibit CYP450 isoforms 1A2, 2C19, 2C9, 2D6 and 3A4 at IC50s > 10 mM in human liver microsomes (HLMs). Use of CYP450 inhibitors show ITMN-191 to be metabolized by multiple CYP450 isoforms. [1]

 

 

 

参考文献

http://www.natap.org/2006/DDW/DDW_30.htm http://www.natap.org/2006/DDW/DDW_30.htm ;

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现货,AEE788,CAS号:497839-62-0,美国进口,受体酪氨酸激酶(RTK) , EGFR , EGFR 抑制剂,selleck,S1486

信号转导通路: 受体酪氨酸激酶(RTK) >> EGFR >> EGFR 抑制剂 >> AEE788http://www.selleck.cn/aee788-S1486.html

技术数据:

分子量(MW): 440.58

化学式:

C27H32N6

 

溶解度: DMSO ≥88mg/mL Water <1mg/mL Ethanol ≥11mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 497839-62-0

生物活性

 

 

AEE788 is a novel multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited with IC50s of 11 and 220 nM, respectively. It efficiently inhibited growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h, a phenomenon correlating with the antitumor efficacy of intermittent treatment schedules. Strikingly, It also inhibited VEGF-induced angiogenesis in a murine implant model. It has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters. [1][2][3]

 

 

 

参考文献

AEE788 : A Dual Family Epidermal Growth Factor Receptor/ErbB2 and Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor with Antitumor and Antiangiogenic Activity Peter Traxler, Peter R. Allegrini,et al. Cancer Res 2004;64:4931-4941

Combining the receptor tyrosine kinase inhibitor AEE788 and the mammalian target of rapamycin (mTOR) inhibitor RAD001 strongly inhibits adhesion and growth of renal cell carcinoma cells Eva Juengel, Johanna Engler,et al. BMC Cancer 2009;9:161

Dual Inhibitor AEE788 Reduces Tumor Growth in Preclinical Models of Medulloblastoma1 Daniela Meco,Tiziana Servidei,et al. Translational Oncology 2010;3:326–335

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现货,Bosutinib (SKI-606) ,CAS号:380843-75-4,美国进口, 受体酪氨酸激酶(RTK) ,SRC ,SRC 抑制剂和化合物,selleck,S1014

信号转导通路: 受体酪氨酸激酶(RTK) >> SRC >> SRC 抑制剂和化合物 >> Bosutinib (SKI-606)http://www.dxy.cn/redirect?url=http://selleck.cn/bosutinib-S1014.html

技术数据:

分子量(MW): 530.45

化学式:

C26H29Cl2N5O3

 

溶解度: DMSO ≥53mg/mL Water <1mg/mL Ethanol ≥24mg/mL

纯度: 99%

稳定性: at -20℃ 2 years

CAS号: 380843-75-4

生物活性

 

 

The cellular Src (c-Src) protein is a nonreceptor tyrosine kinase normally maintained in an inactive conformation via intramolecular interactions.[1] c-Src coordinates multiple signaling pathways known to be involved in tumor progression, such as proliferation, survival, motility, angiogenesis, cell-cell communication, adhesion, and invasion.[2,3] SKI-606 inhibited migration of breast cancer cell lines with IC50 values of 0.1 to 0.3 umol/L; After a 48 h treatment with 1 Amol/L SKI-606, all the invasioncompetent cell lines were unable to cross the porous membrane; cell proliferation and survival were unaffected by SKI-606 at concentrations sufficient to block cell migration and invasion.

 

 

 

参考文献

Src in cancer: deregulation and consequences for cell behaviour Margaret C. Frame Biochimica et Biophysica Acta 2002;1602:114– 130

CELLULAR FUNCTIONS REGULATED BY SRC FAMILY KINASES Sheila M. Thomas,Joan S. Brugge Annu. Rev. Cell Dev. Biol. 1997;13:513–609

Newest findings on the oldest oncogene; how activated src does it Margaret C. Frame Journal of Cell Science 2004;117:989-998

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现货,CP-724714 ,CAS号:537705-08-1,美国进口,受体酪氨酸激酶(RTK), HER2 , HER2 抑制剂,selleck,S1167

信号转导通路: 受体酪氨酸激酶(RTK) >> HER2 >> HER2 抑制剂 >> CP-724714http://www.dxy.cn/redirect?url=http://www.selleck.cn/cp-724714-S1167.html

技术数据:

分子量(MW): 469.53

化学式:

C27H27N5O3

 

溶解度: DMSO ≥94mg/mL Water <1mg/mL Ethanol ≥94mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 537705-08-1

生物活性

 

 

CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor under development for the treatment of advanced HER2-overexpressing cancers. [1]

It inhibits HER2-chimera phosphorylation with an IC50 of 15 ng/ml (32 nM), and is>500-fold selective for HER2 relative to other kinases (e.g. EGFR, PDGFR, IGF-1R, VEGFR-2, abl, src). Antitumor activity of CP-724714 was observed in murine xenografts of human adenocarcinomas of breast (BT-474 and MDAMB-453), pancreas (Panc-1), lung (Calu-3), and ovary (SKOV-3). [1,3]

Additionally, CP-724714 showed a favorable nonclinical toxicity profile with no apparent effects on cardiac tissue. On the basis of these promising preclinical results, CP-724714 was advanced to phase I clinical trials and is potentially another option for women with Her2-driven breast cancer. [2,3]

 

 

 

参考文献

Discovery and Pharmacologic Characterization of CP-724,714, a Selective ErbB2 Tyrosine Kinase Inhibitor Richard S. Finn, Mary Campbell, et al. Cancer Res 2007;67:9887-9893

First Study of the Safety, Tolerability, and Pharmacokinetics of CP-724,714 in Patients with Advanced Malignant Solid HER2-Expressing Tumors Carolyn D. Britten, Monica Mita, et al. Clin Cancer Res 2007;13:1238-1245

Pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors:correlations with clinical characteristics and safety Feng Guo,Stephen P. Letrent,et al. Cancer Chemother Pharmacol 2008;62:97–109

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现货,Masitinib ,CAS号:790299-79-5,美国进口,受体酪氨酸激酶(RTK), c-Kit , c-Kit 抑制剂和化合物,selleck,S1064

信号转导通路:  受体酪氨酸激酶(RTK) >> c-Kit >> c-Kit 抑制剂和化合物 >> 

信号转导通路: 受体酪氨酸激酶(RTK) >> c-Kit >> c-Kit 抑制剂和化合物 >> Masitinibhttp://www.dxy.cn/redirect?url=http://selleck.cn/masitinib-ab1010-S1064.html

技术数据:

分子量(MW): 498.64

化学式:

C28H30N6OS

 

溶解度: DMSO ≥100mg/mL Water <1mg/mL Ethanol ≥4mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 790299-79-5

生物活性

 

 

Masitinib is a tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor with IC50 of 150 ± 80, 200 ± 40 nM for KIT tyrosine phosphorylation and the recombinant human wild-type KIT. It can enhance the antiproliferative effects of gemcitabine (GEM) in human pancreatic cancer cells. It potently inhibited human and murine KIT with activating mutations in the juxtamembrane domain. In vivo, masitinib blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant.[1][2][3]

 

 

 

参考文献

Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT Patrice Dubreuil,Sebastien Letard,et al. PLoS ONE September 2009;4:e7258

Masitinib, a c-kit/PDGF receptor tyrosine kinase inhibitor,improves disease control in severe corticosteroid-dependent asthmatics M. Humbert,F.de Blay,et al. Allergy 2009;64: 1194–1201

Normal and Oncogenic Forms of the Receptor Tyrosine Kinase Kit Johan Lennartsson, Tanya Jelacic,et al. Stem Cells 20

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现货,Flavopiridol (Alvocidib) ,美国进口,黄酮类化合物,细胞周期(Cell Cycle / Checkpoint) ,CDK 抑制剂 ,目录号 S1230

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> CDK >> CDK 抑制剂 >> Flavopiridol (Alvocidib)

技术数据:

分子量(MW): 401.84

化学式:

C21H20ClNO5

 

溶解度: DMSO ≥15mg/mL Water <1mg/mL Ethanol ≥8mg/mL

纯度: >99%

稳定性: -20℃ 2 years

CAS号: 146426-40-6

生物活性

 

 

Nanomolar concentrations of flavopiridol inhibited rhabdoid cell growth (IC50-200nmol/L) , induced G1and G2 arrest, and apoptosis in vitro in a concentration-dependent manner. These effects were correlated with the down-modulation of cyclin D1, up-regulation of p21, and induction of caspase 3/7 activities. Flavopiridol (at 7.5 mg/kg) significantly inhibited the growth of xenografted rhabdoid tumors, and its effect was correlated with the induction of p21 and down-modulation of cyclin D1. [1]

Exposure of HNSCC cells to flavopiridol diminished cdc2 and cdk2 activity and potently inhibited cell proliferation (IC50=43-83 nM), which was concomitant with the appearance of cells with a sub-G1 DNA content. [2]

 

 

 

参考文献

Rhabdoid Tumor Growth is Inhibited by Flavopiridol Velasco Cimica, Srinivasa Chinni, et al. Clin Cancer Res 2008;14:523-532

Flavopiridol, a Novel Cyclin-dependent Kinase Inhibitor, Suppresses the Growth of Head and Neck Squamous Cell Carcinomas by Inducing Apoptosis Vyomesh Patel,Adrian M. Senderowicz,et al. The Journal of Clinical Investigation November 1998;102:1674-1681

现货,Flavopiridol (Alvocidib) ,美国进口,黄酮类化合物,细胞周期(Cell Cycle / Checkpoint) ,CDK 抑制剂 ,目录号 S1230

价  格: 945

说  明: 详询企业QQ4001681698

货  号:S1230

产  地:美国休斯敦

英 文 名:Flavopiridol (Alvocidib)

供 应 商: 赛导通生物科技

规  格:5mg

品  牌:Selleck

保 质 期:两年

保存条件:零下20摄氏度低温保存

CAS号:146426-40-6

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S1230 Flavopiridol (Alvocidib)

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> CDK >> CDK 抑制剂 >> Flavopiridol (Alvocidib)

技术数据:

分子量(MW): 401.84

化学式:

C21H20ClNO5

 

溶解度: DMSO ≥15mg/mL Water <1mg/mL Ethanol ≥8mg/mL

纯度: >99%

稳定性: -20℃ 2 years

CAS号: 146426-40-6

生物活性

 

 

Nanomolar concentrations of flavopiridol inhibited rhabdoid cell growth (IC50-200nmol/L) , induced G1and G2 arrest, and apoptosis in vitro in a concentration-dependent manner. These effects were correlated with the down-modulation of cyclin D1, up-regulation of p21, and induction of caspase 3/7 activities. Flavopiridol (at 7.5 mg/kg) significantly inhibited the growth of xenografted rhabdoid tumors, and its effect was correlated with the induction of p21 and down-modulation of cyclin D1. [1]

Exposure of HNSCC cells to flavopiridol diminished cdc2 and cdk2 activity and potently inhibited cell proliferation (IC50=43-83 nM), which was concomitant with the appearance of cells with a sub-G1 DNA content. [2]

 

 

 

参考文献

Rhabdoid Tumor Growth is Inhibited by Flavopiridol Velasco Cimica, Srinivasa Chinni, et al. Clin Cancer Res 2008;14:523-532

Flavopiridol, a Novel Cyclin-dependent Kinase Inhibitor, Suppresses the Growth of Head and Neck Squamous Cell Carcinomas by Inducing Apoptosis Vyomesh Patel,Adrian M. Senderowicz,et al. The Journal of Clinical Investigation November 1998;102:1674-1681

客户反馈数据

 

(C) In vivo treatment of Tg:Pomc-Pttg;Pomc-eGFP embryos with small-molecule CDK inhibitors (50μM) or 0.2% DMSO as control from 18 to 40 hpf. One hundred to one hundred fifty embryos were treated with each compound. Representative images of live embryos are shown with gross morphology (Right) and pituitary Pomc-GFP–positive cells at higher magnification (Left) at 40 hpf. Embryos exposed to flavopiridol developed early developmental defect before pituitary POMC cell ontogeny occurs. (D) Relative expression of pituitary Pomc-eGFP fluorescence analyzed using Volocity 5.2 software (Improvision; mean ± SE of relative expression, n = 7). (E) R-roscovitine specifically suppresses expansion of pituitary POMC cells overexpressing zPttg from 18 to 48 hpf. Double transgenic Tg:Pomc-Pttg;Prl-RFP embryos were generated by breeding Tg:Pomc-Pttg fish with a previously generated PRL-RFP transgenic line, in which RFP was targeted to pituitary lactotrophs by a zebrafish Prolactin promoter (34). Representative fluorescent microscopy of pituitary POMC-eGFP (a and b) and PRL-RFP (c and d) expression in live Tg:Pomc-Pttg; Pomc-eGFP and Tg:Pomc-Pttg;Prl-RFP embryos treated with 0.2% DMSO (a and c) or 50 μM R-roscovitine (b and d). (F) Relative expression of pituitary POMC-eGFP or PRL-RFP fluorescence were analyzed (mean ± SE of relative expression; n = 10). Results represent one of three similar experiments;*P < 0.02 and **P < 0.000005. (Scale bar, 50 μm.)

 

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现货,NPI-2358 (Plinabulin) ,CAS号:714272-27-2,美国进口,血管生成(Angiogenesis) , VDA , VDA 抑制剂,selleck,S1176

信号转导通路: 血管生成(Angiogenesis) >> VDA >> VDA 抑制剂 >> NPI-2358 (Plinabulin)http://selleck.cn/npi-2358-S1176.html

技术数据:

分子量(MW): 336.39

化学式:

C19H20N4O2

 

溶解度: DMSO ≥67mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 714272-27-2

生物活性

 

 

NPI-2358 (Plinabulin) is a novel vascular disrupting agent (VDA) with an IC50 of 15 nM against HT-29 cells. NPI-2358 binds to the colchicine-binding site of tubulin. NPI-2358 has potent in-vitro anti-tumor activity against various human tumor cell lines and maintains activity against tumor cell lines with various MDR profiles. In addition, when evaluated in proliferating human umbilical vein endothelial cells (HUVECs), concentrations as low as 10 nmol/l NPI-2358 induced tubulin depolymerization within 30 min. Furthermore, NPI-2358 dose dependently increases HUVEC monolayer permeability--an in-vitro model of tumor vascular collapse. NPI-2358 blocks growth and angiogenesis in multiple myeloma cells

NPI-2358 acts on tubulin dimerization that destabilizes tumor vascular endothelial cells and has cytotoxic activity (IC50 values of 10-15 nM). NPI-2358 selectively induces tumor vascular collapse and tumor regression in murine tumor models and potentiates other oncology agents. Preclinical data suggest NPI-2358 may have advantages in terms of safety profile and activity. [1][2]

 

 

 

参考文献

Phase I study of NPI-2358 (a novel vascular disrupting agent) in patients with solid tumors and lymphomas. A. C. Mita, et al. J Clin Oncol. 2008;

NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. Nicholson B, et al. Anticancer Drugs. 2006 Jan;;17(1):25-31.

客户反馈数据

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现货,MLN2238,CAS号:1072833-77-2,美国进口,蛋白酶体(Proteases),Proteasome , Proteasome 抑制剂,selleck,S2180

信号转导通路: 蛋白酶体(Proteases) >> Proteasome >> Proteasome 抑制剂 >> MLN2238http://www.selleck.cn/mln-2238-S2180.html

技术数据:

分子量(MW): 361.03

化学式:

C14H19BCl2N2O4

 

溶解度: DMSO ≥72mg/mL Water <1mg/mL Ethanol ≥9mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1072833-77-2

生物活性

 

 

MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM. Proteasome activity was significantly inhibited in both blood and tumor following a single dose of MLN2238 administered IV at 14 mg/kg or SC at 4 mg/kg. Proteasome activity was inhibited greater than 50% for up to 8 hrs following the IV dose in both blood and tumor, whereas proteasome activity recovered more quickly following the SC dose. It is active in preclinical models of lymphoma, and that MLN2238 has antitumor activity in a model of lymphoma that is refractory to bortezomib treatment. [1][2]

 

 

 

参考文献

http://ash.confex.com/ash/2009/webprogram/Paper20088.html http://ash.confex.com/ash/2009/webprogram/Paper20088.html ;

http://ash.confex.com/ash/2009/webprogram/Paper19135.html http://ash.confex.com/ash/2009/webprogram/Paper19135.html ;

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现货,Aurora A Inhibitor I ,CAS号:1158838-45-9,美国进口, HDAC-HSP-Aurora , Aurora Kinase, Aurora Kinase 抑制剂和化合物

信号转导通路:  细胞周期(Cell Cycle / Checkpoint) >> PARP >> PARP 抑制剂和化合物 >> 

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> PARP >> PARP 抑制剂和化合物 >> AG14361http://www.dxy.cn/redirect?url=http://selleck.cn/aurora-a-inhibitor-i-S1451.html

技术数据:

分子量(MW): 320.39

化学式:

C19H20N4O

 

溶解度: DMSO ≥21mg/mL Water <1mg/mL Ethanol ≥12mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 328543-09-5

生物活性

 

 

AG14361 is a potent poly(ADP-ribose) polymerase (PARP-1) inhibitor with a GI50 of 10.9 µM. It caused a >3-fold sensitization of PARP-1+/+ cells to topotecan compared with a <1.4-fold sensitization in PARP-1−/− cells. In human leukemia K562 cells, AG14361 caused a 2-fold sensitization to camptothecin-induced cytotoxicity. AG14361 did not affect the cellular activity of topo I as determined by measurement of cleavable complexes and topo I relaxation activity, showing that sensitization was not due to topo I activation. [1][2][3]

 

 

 

参考文献

Anticancer Chemosensitization and Radiosensitization by the Novel Poly(ADP-ribose) Polymerase-1 Inhibitor AG14361 Christopher R. Calabrese, Robert Almassy,et al. Journal of the National Cancer Institute January 7, 2004;96:56-67

The Novel Poly(ADP-Ribose) Polymerase Inhibitor, AG14361,Sensitizes Cells to Topoisomerase I Poisons by Increasing the Persistence of DNA Strand Breaks Elaine Willmore, Caroline A. Austin, et al. Clin Cancer Res 2005;11:8449-8457

Novel Poly(ADP-ribose) Polymerase-1 Inhibitor, AG14361,Restores Sensitivity to Temozolomide in Mismatch Repair-Deficient Cells Lan-Zhen Wang, Anthie Yiakouvaki, et al. Clin Cancer Res 2004;10:881-889

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现货,Staurosporine ,CAS号:62996-74-1,美国进口, TGF-beta / smad , PKC,selleck,S1421

信号转导通路: TGF-beta / smad >> PKC >> PKC 抑制剂 >> Staurosporinehttp://www.selleck.cn/staurosporine-S1421.html

技术数据:

分子量(MW): 466.53

化学式:

C28H26N4O3

 

溶解度:

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 62996-74-1

生物活性

 

 

Staurosporine is a prototypical potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. The interest in these activities resulted in a large investigative effort in chemistry and biology and the discovery of the potential for anti-cancer treatment. Staurosporine induces apoptosis in human neuroblastoma cell lines and chick embryonic neurons. Staurosporine is a natural product originally isolated from the bacterium Streptomyces staurosporeus. [1][2]

 

 

 

参考文献

STAUROSPORINE, A PROTEIN KINASE C INHIBITOR INTERFERES WITH PROLIFERATION OF ARTERIAL SMOOTH MUSCLE CELLS Hiroaki Matsumoto and Yasuharu Sasaki BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS January 16, 1989 ;158:105-109

STAUROSPORINE, A POTENT INHIBITOR OF PHOSPHOLIPID/Ca++DEPENDENT PROTEIN KINASE Tatsuya Tamaoki,Hisayo Nomoto,et al. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS March 13,1986 ;135:397-402

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现货,CYT997,CAS号:917111-44-5,美国进口,细胞周期(Cell Cycle / Checkpoint) , Microtubule Formation ,selleck,目录号S2195

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> Microtubule Formation >> Microtubule Formation 抑制剂 >> CYT997http://www.selleck.cn/cyt997-S2195.html

技术数据:

分子量(MW): 434.53

化学式:

C24H30N6O2

 

溶解度: DMSO ≥87mg/mL Water <1mg/mL Ethanol ≥20mg/mL

纯度: >95%

稳定性: at -20℃ 2 years

CAS号: 917111-44-5

生物活性

 

 

CYT997, a synthetic small molecule optimized for antiproliferative activity in a panel of cell-based assays, in which the compound shows an IC50 of between 1 and 100 nmol/L across a panel of cancer cell lines. The compound inhibits the polymerization of tubulin with an IC50 of ~3 μmol/L.CYT997 causes a significant increase of cells in the G2-M phase of the cell cycle.Caspase-3 activation is also observed in cells treated with CYT997 along with the generation of poly(ADP-ribose) polymerase.CYT997 exhibits vascular disrupting activity as measured in vitro by effects on the permeability of human umbilical vein endothelial cell monolayers, and in vivo by effects on tumor blood flow. CYT997 possesses a useful combination of pharmacologic and pharmacokinetic properties and has considerable potential as a novel anticancer agent. [1]

 

 

 

参考文献

CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vivo and in vitro Emmanuelle Fantino, Ian D. Phillips, et al. Mol Cancer Ther 2009;8:3036-3045

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现货,GSK1059615 ,CAS号:958852-01-2,美国进口,PI3K / mTOR / AKT , PI3K,PI3K 抑制剂,selleck,目录号S1360

信号转导通路: PI3K / mTOR / AKT >> PI3K >> PI3K 抑制剂 >> GSK1059615http://www.dxy.cn/redirect?url=http://www.selleck.cn/gsk1059615-S1360.html

技术数据:

分子量(MW): 333.36

化学式:

C18H11N3O2S

 

溶解度: DMSO ≥5mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 958852-01-2

生物活性

 

 

GSK1059615 is a pan-PI3K reversible inhibitor with sub-nanomolar IC50 for PI3Kα (0.4 nM) and PI3Kβ (0.6 nM) and shows low nanomolar activity towards γ(5 nM),δ(2 nM) and mTOR(12 nM). GSK1059615 inhibits PI3K pathway in cells inducing G1 arrest, although apopto-sis was observed in a subset of cell lines. Breast tumor cells seem to be more sensitive to this compound. In xenograft mice, a complete tumor inhibition and regression were observed together with an increase in plasma insulin levels. [1]

 

 

 

参考文献

Novel inhibitors of the PI3K family Informa healthcare September 2009;1265-1277

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现货,WYE-354 ,CAS号:1062169-56-5,美国进口,PI3K / mTOR / AKT , mTOR ,mTOR 抑制剂,selleck,目录号S1266

信号转导通路:  PI3K / mTOR / AKT >> mTOR >> mTOR 抑制剂 >> 

信号转导通路: PI3K / mTOR / AKT >> mTOR >> mTOR 抑制剂 >> WYE-354http://www.dxy.cn/redirect?url=http://www.selleck.cn/wye-354-S1266.html

技术数据:

分子量(MW): 495.53

化学式:

C24H29N7O5

 

溶解度: DMSO ≥99mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1062169-56-5

生物活性

 

 

WYE-354,a cell-permeable pyrazolopyrimidine compound,is a potent and ATP competitive inhibitor of mTOR (IC50 = 5 nM), with significant selectivity over PI3K isofoms (>100-fold). When injected into tumor-bearing nude mice, WYE-354 inhibited mTORC1 and mTORC2 and displayed robust antitumor activity in PTEN-null tumors. [1]

 

 

 

参考文献

Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin Lourdes Toral-Barza, Celine Shi, et al. Cancer Res 2009;69:6232-6240

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现货,NVP-AEW541 ,CAS号:475489-16-8,美国进口,受体酪氨酸激酶(RTK) , IGF-1R, IGF-1R 抑制剂和化合物

信号转导通路: 受体酪氨酸激酶(RTK) >> IGF-1R >> IGF-1R 抑制剂和化合物 >> NVP-AEW541http://selleck.cn/nvp-aew541-S1034.html

技术数据:

分子量(MW): 439.55

化学式:

C27H29N5O

 

溶解度: DMSO ≥88mg/mL Water <1mg/mL Ethanol ≥88mg/mL

纯度: 99%

稳定性: at -20℃ 2 years

CAS号: 475489-16-8

生物活性

 

 

NVP-AEW541 is an IGF-IR inhibitor with an IC50 of median 3.6 μM.

NVP-AEW541 is a pyrrolo[2,3-d]pyrimidine derivative highly selective against IGF-IR, compared with the insulin receptor and other tyrosine kinases. In a panel of 10 neuroblastoma cell lines positive for IGF-IR expression, NVP-AEW541 inhibited in vitro proliferation in a submicromolar/micromolar (0.4-6.8) range of concentrations. NVP-AEW541 inhibits IGF-I-mediated receptor activation and downstream signaling. In addition to growth inhibition, NVP-AEW541 also induced apoptosis in vitro. Oral administration of NVP-AEW541 (50 mg/kg twice daily) inhibited tumor growth of neuroblastoma xenografts in nude mice. Therapeutic potential of NVP-AEW541 was also analyzed in Ewing’s sarcoma, osteosarcoma, rhabdomyosarcoma, and pancreatic cancer. [1][2]

 

 

 

参考文献

Down-Regulation of Insulin-Like Growth Factor I Receptor Activity by NVP-AEW541 Has an Antitumor Effect on Neuroblastoma Cells In vivo and In vitro Camillo Mancini, Roberta Vitali, et al. Clin Cancer Res 2006;12:6772-6780

Antitumor Activity of the Insulin-Like Growth Factor-I Receptor Kinase Inhibitor NVP-AEW541 in Musculoskeletal Tumors Maria Cristina Manara, Giordano Nicoletti, et al. Cancer Res 2005;65:3868-3876

 

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现货,Dapagliflozin,CAS号:461432-26-8,美国进口,G蛋白偶联受体(GPCR & G P) , SGLT , SGLT 抑制剂和化合物,selleck,S1548

信号转导通路: G蛋白偶联受体(GPCR & G P) >> SGLT >> SGLT 抑制剂和化合物 >> Dapagliflozinhttp://www.dxy.cn/redirect?url=http://selleck.cn/dapagliflozin-S1548.html

技术数据:

分子量(MW): 408.87

化学式:

C21H25ClO6

 

溶解度: DMSO ≥82mg/mL Water <1mg/mL Ethanol ≥82mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 461432-26-8

生物活性

 

 

Dapagliflozin(BMS-512148) is a potent sodium-glucose transport proteins inhibitor with IC50 of 1.1 nM and 1.4 μM for SGLT2 and SGLT1, respectively. Dapagliflozin (BMS-512148) inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Symptoms of hypoglycaemia occurred in similar proportions of patients in the dapagliflozin (2~4%) and placebo groups (3%). Signs, symptoms, and other reports suggestive of genital infections were more frequent in the dapagliflozin groups (2•5 mg, [8%]; 5 mg, [13%]; 10 mg, [9%]) than in the placebo group ( [5%]). [1][2][3]

 

 

 

参考文献

Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin:a randomised, double-blind, placebo-controlled trial Cliff ord J Bailey, Jorge L Gross, et al. Lancet 2010;375: 2223–2233

In Vitro Characterization and Pharmacokinetics of Dapagliflozin (BMS-512148), a Potent Sodium-Glucose Cotransporter Type II Inhibitor, in Animals and Humans M. Obermeier, M. Yao,et al. DMD 2010;38:405–414

客户反馈数据

如果需要长期保存,请于零下二十度低温保存。

禁止用于人体及治疗!

特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20 ° C ,抗体及蛋白等产品建议-60℃。抑制剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。

 

 

 

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现货,BIRB 796 (Doramapimod),CAS号:285983-48-4,美国进口,MAPK, p38 MAPK , p38 MAPK 抑制剂,selleck,S1574

信号转导通路: MAPK >> p38 MAPK >> p38 MAPK 抑制剂 >> BIRB 796 (Doramapimod)http://www.dxy.cn/redirect?url=http://www.selleck.cn/birb-796-doramapimod-S1574.html

技术数据:

分子量(MW): 527.66

化学式:

C31H37N5O3

 

溶解度: DMSO ≥106mg/mL Water <1mg/mL Ethanol ≥106mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 285983-48-4

生物活性

 

 

BIRB796有效抑制p38 MAPK。在体外,由于慢性结合和分裂行为, BIRB796作用于纯化的P38 MAPK,随着预温育的时间从8分钟到120分钟不等,IC50值也在97nM到8nM范围之间变化。[1] BIRB796对炎症和一些癌细胞非常有效。[2] BIRB796二期临床试验的完成用于治疗克罗恩氏病和银屑病,但是目前还没有更进一步的发展。[3]BIRB796最初是由Boehringer Ingelheim 研究的。

 

 

 

信号转导通路: MAPK >> p38 MAPK >> p38 MAPK 抑制剂 >> BIRB 796 (Doramapimod)http://www.dxy.cn/redirect?url=http://www.selleck.cn/birb-796-doramapimod-S1574.html

技术数据:

分子量(MW): 527.66

化学式:

C31H37N5O3

 

溶解度: DMSO ≥106mg/mL Water <1mg/mL Ethanol ≥106mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 285983-48-4

生物活性

 

 

BIRB796有效抑制p38 MAPK。在体外,由于慢性结合和分裂行为, BIRB796作用于纯化的P38 MAPK,随着预温育的时间从8分钟到120分钟不等,IC50值也在97nM到8nM范围之间变化。[1] BIRB796对炎症和一些癌细胞非常有效。[2] BIRB796二期临床试验的完成用于治疗克罗恩氏病和银屑病,但是目前还没有更进一步的发展。[3]BIRB796最初是由Boehringer Ingelheim 研究的。

 

 

 

参考文献

[1] Nat. Struct. Biol. 2002, 9, 268-272.

[2] J. Boil. Chem. 2005, 280, 19472-19479.

[3] Biochemistry.2010 May 4;49(17):3611-8

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现货,LY2140023 (LY404039) ,CAS号: 635318-11-5 ,美国进口, 神经信号通路(Neuronal Signaling) , mGluR,mGluR 抑制剂,selleck,S6001

信号转导通路: 神经信号通路(Neuronal Signaling) >> mGluR >> mGluR 抑制剂 >> LY2140023 (LY404039)http://selleck.cn/ly2140023-ly404039-S6001.html

技术数据:

分子量(MW): 235.22

化学式:

C7H9NO6S

溶解度: DMSO ≥1mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 635318-11-5

生物活性

 

LY2140023 (LY404039) is a selective metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3 agonist with Ki of 149 and 92nM for mGlu2 and mGlu3, respectively.Functional activity of LY2140023 (LY404039) at group II and group III mGlu receptors is measured by the inhibition of forskolin-stimulated cAMP formation. It is nanomolar potent agonists at human mGlu2 and mGlu3 receptors, as indicated by the inhibition of forskolin-stimulated cAMP formation (LY404039: mGlu2, EC50 =23 nM; mGlu3, EC50 = 48 nM). It suppressed the frequency of 5-HT-induced EPSCs with an EC50 of 82.3 nM and with a near maximal suppression of 85.6% at 1 μM. Intraperitoneal administration of LY2140023 (LY404039) (10 mg/kg) to wild-type mice significantly inhibited increases evoked by PCP (7.5 mg/kg) in ambulations. It produced a dose-dependent reduction of increases evoked by AMP (5 mg/kg) in ambulations. [1][2]

 

参考文献

Pharmacological and Pharmacokinetic Properties of a Structurally Novel, Potent, and Selective Metabotropic Glutamate 2/3 Receptor Agonist: In Vitro Characterization of Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic Acid (LY404039) Linda M. Rorick-Kehn, Bryan G. Johnson,et al. JPET 2007;321:308–317

Evidence for the Role of Metabotropic Glutamate (mGlu)2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039) Matthew J. Fell, Kjell A. Svensson,et al. JPET 2008;326:209–217

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现货,TW-37 ,CAS号:877877-35-5,美国进口,细胞凋亡(Apoptosis) ,Bcl-2, Bcl-2 抑制剂 ,目录号S1121

信号转导通路: 细胞凋亡(Apoptosis) >> Bcl-2 >> Bcl-2 抑制剂 >> TW-37http://www.dxy.cn/redirect?url=http://www.selleck.cn/tw-37-S1121.html

技术数据:

分子量(MW): 573.7

化学式:

C33H35NO6S

 

溶解度: DMSO ≥115mg/mL Water <1mg/mL Ethanol ≥4mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 877877-35-5

生物活性

 

 

TW-37 is a Bcl-2 protein family inhibitor with a Ki of 0.29 μM. TW-37 binds to the BH3 binding groove in Bcl-2 protein competing with BH3 peptides derived from Bid, Bim, and Bad proteins. TW-37 binds to Bcl-2 with a Ki value of 290 nM and also to Bcl-xL and Mcl-1 with high affinities. TW-37 potently inhibits cell growth in PC-3 prostate cancer cells with an IC50 value of 200 nM and effectively induces apoptosis in a dose-dependent manner. TW-37 has an IC50 of 1.1 μM for primary human endothelial cells and averaged 0.3 μM for head and neck cancer cells (OSCC3, UM-SCC-1, and UMSCC-74A). The combination of TW-37 and cisplatin showed enhanced cytotoxic effects for endothelial cells and HNSCC in vitro, compared with single agent treatment. [1][2]

 

 

 

参考文献

Antiangiogenic Effect of TW37, a Small-Molecule Inhibitor of Bcl-2 Esther Joo, Zhihong Dong, et al. Cancer Res 2006;66:8698-8706

TW-37, a small-molecule inhibitor of Bcl-2, mediates S-phase cell cycle arrest and suppresses head and neck tumor angiogenesis Benjamin D. Zeitlin, Zhaocheng Zhang, et al. Mol Cancer Ther 2009;8:893-903

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