现货,YM155,细胞凋亡(Apoptosis),CAS号:781661-94-7,美国进口, Survivin ,Survivin 抑制剂,S1130,selleck

信号转导通路: 细胞凋亡(Apoptosis) >> Survivin >> Survivin 抑制剂 >> YM155http://selleck.cn/ym155-S1130.html

技术数据:

分子量(MW): 443.29

化学式:

C20H19BrN4O3

 

溶解度: DMSO ≥89mg/mL Water ≥89mg/mL Ethanol ≥24mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 781661-94-7

生物活性

 

 

YM155 is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity. However, YM155 (YM 155, YM-155) did not significantly inhibit SV40 promoter activity at concentrations up to 30 μM. YM155 (YM 155, YM-155) induced apoptosis in PC-3 and PPC-1 human HRPC cell lines at 10 nM. In a s.c.xenografted PC-3 tumor model in mice, 3-day continuous infusions of YM155 (YM 155, YM-155) at 3 to 10 mg/kg induced massive tumor regression accompanied by suppression of intratumoral survivin. Pharmacokinetic analyses indicated that YM155 (YM 155, YM-155) is highly distributed to tumors and at concentrations approximately 20-fold higher than those in plasma. [1][2][3]

 

 

 

参考文献

YM155, a Novel Small-Molecule Survivin Suppressant,Induces Regression of Established Human Hormone-Refractory Prostate Tumor Xenografts Masahiro Takeuchi, Isao Kinoyama, et al. Cancer Res 2007;67:8014-8021

Multicenter Phase II Trial of YM155, a Small-Molecule Suppressor of Survivin, in PatientsWith Advanced,Refractory, Non–Small-Cell Lung Cancer Giuseppe Giaccone, Petr Zatloukal,et al. J Clin Oncol 2009;27:4481-4486.

Phase I and Pharmacokinetic Study of YM155, a Small-Molecule Inhibitor of Survivin Anthony W. Tolcher, Alain Mita,et al. J Clin Oncol 2008;26:5198-5203

 

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