| 产品详情 |
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| Product Name | PHA-665752 |
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| Description | Purity >98%. The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers. PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM; IC50 = 9 nM). 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 (IC50 s = 18-50 nM). It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-Gamma, and focal adhesion kinase in multiple tumor cell lines. In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation. |
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| Size | n/a |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | (3Z)-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-2H-indol-2-one |
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| Gene, Accession, CAS # | CAS: 477575-56-7 |
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| Catalog # | LS-H9364 |
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| Order / More Info | PHA-665752 from LIFESPAN BIOSCIENCES INC. |
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| Product Specific References | n/a |
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