|2-(4-(1-(喹啉-6-基甲基)-1H-[1,2,3]三唑并[4,5-b]吡嗪-6-基)-1H-吡唑-1-基)乙-1-醇甲磺酸盐|CsnPharm

CAS No.: 956906-93-7

2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethan-1-ol methanesulfonate Catalog No. CSN18635

Synonyms: PF-04217903 mesylate;PF-04217903;PF-4217903

PF-04217903 Methanesulfonate is a highlu selective c-Met inhibitor with IC50 of 4.8 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 c-Met

IC50:4.8nM
描述c-Met is the prototypical member of a subfamily of RTKs (receptor tyrosine kinases). Hepatocyte growth factor (HGF) is the only known high-affinity ligand of c-Met. Activation of the c-Met pathway provides a powerful signal for cell survival, migration, and proliferation (invasive growth). PF-04217903 is a potent and selective ATP-competitive inhibitor of the catalytic activity of recombinant, human c-Met kinase with a mean K_i of 4.8 nM. In cell-based assays, PF-04217903 inhibited HGF-stimulated or constitutive total tyrosine phosphorylation of wild type c-Met with a mean IC₅₀ value of 7.3 nM across a panel of human tumor and endothelial cell line including GTL-16, H1993, and HT29 cells. PF-04217903 inhibited proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC₅₀ values of 12 and 30 nM, respectively and induced apoptosis of GTL-16 cells with an IC₅₀ of 31 nM. PF-04217903 also inhibited HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines with IC₅₀ values among 7–12.5 nM. In c-Met–amplified GTL-16 model, PF-04217903 showed dose-dependent tumor growth inhibition (TGI), which correlated with the inhibition in c-Met phosphorylation in these tumors. Moreover, 5 hours after oral dosing, PF-04217903 dose dependently inhibited c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels (5, 15, and 50 mg/kg, orally/once daily for 3 days)^[3].
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.
[3] Zou HY, Li Q, Lee JH, et, al. Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor. Mol Cancer Ther. 2012 Apr;11(4):1036-47

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1345 mL
- 10.6726 mL
- 21.3452 mL
- 5 mM
- 0.4269 mL
- 2.1345 mL
- 4.2690 mL
- 10 mM
- 0.2135 mL
- 1.0673 mL
- 2.1345 mL

技术信息

CAS号

956906-93-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H20N8O4S

运输

蓝冰

分子量

468.49

别名

PF-04217903 mesylate;PF-04217903;PF-4217903

溶解度

DMSO	50.0 mg/mL (106.7 mM) warming
Water	Insoluble

动物实验配方

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2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethan-1-ol methanesulfonate Catalog No. CSN18635

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