现货,AT9283 ,CAS:896466-04-9,美国进口,受体酪氨酸激酶(RTK) ,Bcr-Abl , Bcr-Abl 抑制剂和化合物,S1134,selleck

信号转导通路: 受体酪氨酸激酶(RTK) >> Bcr-Abl >> Bcr-Abl 抑制剂和化合物 >> AT9283http://www.dxy.cn/redirect?url=http://selleck.cn/at9283-S1134.html

技术数据:

分子量(MW): 381.43

化学式:

C19H23N7O2

 

溶解度: DMSO ≥76mg/mL Water <1mg/mL Ethanol ≥28mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 896466-04-9

生物活性

 

 

AT9283 is a small molecule a multi-targeted c-ABL, JAK2, Aurora A and B inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively. AT9283 inhibited growth and survival of multiple solid tumor cell lines and was efficacious in mouse xenograft models. AT9283-treatment resulted in endoreduplication and ablation of serine-10 histone H3 phosphorylation in both cells and tumor samples. AT9283 demonstrated in vivo efficacy in mouse xenograft models and is currently under evaluation in phase I clinical trial. AT9283 showed potent antiproliferative activity on cells transformed by wild-type BCR-ABL and BCR-ABL/T315I. AT9283 inhibited proliferation in a panel of BaF3 and human BCR-ABL+ cell lines both sensitive and resistant to imatinib because of a variety of mechanisms. In BCR-ABL+ cells, inhibition of substrates of both BCR-ABL (signal transducer and activator of transcription-5) and Aurora B (histone H3) at physiologically achievable concentrations was confirmed. [1][2][3]

 

 

 

参考文献

Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity Steven Howard,Valerio Berdini,et al. J. Med. Chem 2009;52:379–388

Aurora B kinase inhibition in mitosis Jayne Curry,Hayley Angove,et al. Cell Cycle 15 June 2009;8:12,1921-1929

Activity of the multitargeted kinase inhibitor, AT9283, in imatinib-resistant BCR-ABL positive leukemic cells Ruriko Tanaka, Matthew S. Squires,et al. Blood 2010;116: 2089-2095

退换货政策

1、 退换货只针对已付款用户。一张订单Selleck只提供一次退换货服务,为了确保您的权益,请考虑周全后与我们联系。

2、请您确保退换货时,商品、配件、赠品及各种包装完整。

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。

 

Write a comment

Comments: 0



赛导通生物科技联系方式:


上海市黄浦区江西中路261号509室,

近南京东路外滩


电话 400-168-1698


传真 021 3326 0586


邮箱: info@selleck.cn 

 技术: tech@selleck.cn



Selleck癌症肿瘤研究周刊


Stu.la 司途拉生物
Stu.la 司途拉生物