PHA-665752
货号：
14703-1mg 基本售价：
546.0 元 规格：
1 mg
产品信息
概述| 货号 | 14703-1mg |
| 描述 | The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers.1 PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM; IC50 = 9 nM).2 It exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. PHA-665752 can inhibit c-Met phosphorylation, as well as cell proliferation and cell motility, of various tumor cells (IC50s = 18-50 nM).2 It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-γ, and focal adhesion kinase in multiple tumor cell lines.2 In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Mughal, A.,Aslam, H.M.,Sheikh, A., et al. c-Met inhibitors. Infect.Agent.Cancer 8, 13 (2013).
2.Christensen, J.G.,Schreck, R.,Burrows, J., et al. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Research 63(21), 7345-7355 (2003).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 641.6 |
| 分子式 | C32H34Cl2N4O4S |
| CAS号 | 477575-56-7 |
| 稳定性 | ≥ 2 years |
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