PF-04217903

≥98%

PF-04217903

产品说明书 SDS 产品使用指南

品牌：源叶(MedMol)

产品编号：S81578 一键复制产品信息

CAS号：956905-27-4

分子式：C₁₉H₁₆N₈O

分子量：372.38

别名：PF 04217903;2-[4-[1-(喹啉-6-甲基)-1H-[1,2,3]三唑并[4,5-b]吡嗪-6-基]-1H-吡唑-1-基]乙醇

货号	规格	价格	上海	北京	珠海	重庆	武汉
S81578-2mg促销	≥98%	￥315.00 ￥282.00 S81578-2mg ￥282.00 3-5天	0 货期：3-5天	-	-	-	-
S81578-5mg促销	≥98%	￥565.00 ￥508.00 S81578-5mg ￥508.00 现货	10 10	2	1	-	-
S81578-10mg促销	≥98%	￥1000.00 ￥900.00 S81578-10mg ￥900.00 现货	6 6	3	-	-	-
S81578-50mg促销	≥98%	￥2700.00 ￥2430.00 S81578-50mg ￥2430.00 3-5天	0 货期：3-5天	-	1	-	-

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产品介绍参考文献质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties

靶点：

Ki: 4.8 nM (human c-Met);c-Met/HGFR

体内研究：

PF-04217903 (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors. PF-04217903 (5-50 mg/kg, p.o.; once daily for 3 days) dose dependently inhibits c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels. PF-04217903 phenolsulfonate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors

参考文献：

1. Zou HY, 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. 2. Cui JJ, et al. Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl) 3. Timofeevski SL, et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry, 2009, 48(23), 5339-5349.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.685 ml	13.427 ml	26.854 ml
5 mM	0.537 ml	2.685 ml	5.371 ml
10 mM	0.269 ml	1.343 ml	2.685 ml
50 mM	0.054 ml	0.269 ml	0.537 ml