貨號	規格	價格	上海	北京	武漢	南京
S81578-2mg	≥98%	￥314.00 S81578-2mg ￥314.00 2-3天	0 貨期：2-3天	-	-	-
S81578-5mg	≥98%	￥564.00 S81578-5mg ￥564.00 現貨	10 10	-	-	-
S81578-10mg	≥98%	￥1000.00 S81578-10mg ￥1000.00 現貨	6 6	-	-	-
S81578-50mg	≥98%	￥4900.00 S81578-50mg ￥4900.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

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

靶點：

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

體內研究：

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

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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