(3Z)-5-((2,6-Dichlorobenzyl)sulfonyl)-3-((3,5-dimethyl-4-(((2R)-2-(pyrrodin-1-ylmethyl)pyrrolidin-1-yl)carbonyl)-1H-pyrrol-2-yl)methylene)-1,3-dihydro-2H-indol-2-one
PHA665752 Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable pyrrolo-indolinone compound that acts as an ATP-competitive and highly potent inhibitor of c-Met tyrosine kinase activity (IC50= 9 nM) with good selectivity in both cell-free kinase assays (7.5-, 22-, 155-, and ≥333-fold over Ron, Flk1, c-abl, and a panel of 12 other commonly studied kinases, respectively) and in receptor autophosphorylation in cells (20- and 60-fold over Ron and Flk1, respectively). Shown to suppress c-Met-mediated cellular functions in vitro and inhibit tumorigenicity in various murine tumor models in vivo. Purity: ≥98% by HPLC. CAS 477575-56-7. Ref.: Puri, N., et al. 2007. Cancer Res. 67, 3529. Christensen, J.G., et al. 2003. Cancer Res. 63, 7345.
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