产品说明书

PF-04217903

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Chemical Structure| 956905-27-4 同义名 : -
CAS号 : 956905-27-4
货号 : A670353
分子式 : C19H16N8O
纯度 : 99%+
分子量 : 372.383
MDL号 : MFCD12407410
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(48.34 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+2% Tween 80+water 2 mg/mL

生物活性
描述 PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A549 cells Function assay 1 h Antagonist activity at c-MET receptor in human A549 cells assessed as inhibition of autophosphorylation after 1 hr by ELISA, IC50=4 nM 22924734
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.43mL

2.69mL

1.34mL

26.85mL

5.37mL

2.69mL
参考文献

[1]Shojaei F, Lee JH, et al. HGF/c-Met acts as an alternative angiogenic pathway in sunitinib-resistant tumors. Cancer Res. 2010 Dec 15;70(24):10090-100.

[2]Timofeevski SL, McTigue MA, et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry. 2009 Jun 16;48(23):5339-49.