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Chemical Structure : PHA-665752
CAS No.: 477575-56-7
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $168 | In stock | |
| 50 mg | $268 | In stock | |
| 100 mg | $458 | In stock | |
| 500 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 641.6078 | |
| Formula | C32H34Cl2N4O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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)- |
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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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