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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Met (HGFR)-PHA-665752
PHA-665752

Chemical Structure : PHA-665752

CAS No.: 477575-56-7

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PHA-665752 (PHA 665752;PHA665752)

货号: PC-42814Not For Human Use, Lab Use Only.

PHA-665752 is a potent, selective, ATP-competitive c-Met inhibitor with Ki/IC50 of 4/9 nM, inhibits c-Met RTK autophosphorylation in A549 cells with IC50 of 45 nM.

规格 价格 库存 数量
25 mg ￥1680 In stock
50 mg ￥2680 In stock
100 mg ￥4580 In stock
500 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PHA-665752 is a potent, selective, ATP-competitive c-Met inhibitor with Ki/IC50 of 4/9 nM, inhibits c-Met RTK autophosphorylation in A549 cells with IC50 of 45 nM.
PHA-665752 exhibits >50-fold selectivity for c-Met against a panel of kinases with exceptions of Ron and VEGFR2 (IC50=68 and 200 nM).
PHA-665752 inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream signal transduction of c-Met, including Gab-1, ERK, Akt, STAT3, PLCγ, and FAK in multiple tumor cell lines.
PHA-665752 inhibits c-Met phosphorylation and tumor growth in vivo.

物理化学性质&存储条件

分子量 641.6078
分子式 C32H34Cl2N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2H-Indol-2-one, 5-[[(2,6-dichlorophenyl)methyl]sulfonyl]-3-[[3,5-dimethyl-4-[[(2R)-2-(1-pyrrolidinylmethyl)-1-pyrrolidinyl]carbonyl]-1H-pyrrol-2-yl]methylene]-1,3-dihydro-, (3Z)-

参考文献

1. Smolen GA, et al. Proc Natl Acad Sci U S A. 2006 Feb 14;103(7):2316-21.

2. Ma PC, et al. Clin Cancer Res. 2005 Mar 15;11(6):2312-9.

3. Hov H, et al. Clin Cancer Res. 2004 Oct 1;10(19):6686-94.

4. Christensen JG, et al. Cancer Res. 2003 Nov 1;63(21):7345-55.

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