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AMG-337
AMG-337 is an orally bioavailable, potent and exquisitely selective inhibitor of wild-type and some mutant forms of c-Met. In competitive binding assays on 402 human kinases, enantiomerically (optically) pure AMG-337 hits c-Met only (with an IC50 < 5 nM). In a cell viability study, the only cell lines that responded to an AMG 337 were gastric cancer cells harboring c-Met gene amplification. None of the other cell lines were sensitive to the AMG-337 and none harbored c-Met gene amplification. It inhibited HGF-dependent c-Met phosphorylation with an IC50 of less than 10 nM in cellular assay. Orally administered AMG-337 in c-Met amplified gastric cancer xenograft models resulted in a robust dose-dependent anti-tumor efficacy.
Catalog NO: CT-AMG337
Synonym: AMG337
CAS NO: 1173699-31-4
Mol. Formula: C23H22FN7O3 ∙ 0.5H2O
MW: 472.5
** A white powder (with faint yellow tint), recrystallized, clean (>99.5% chemically pure by HPLC), optically pure (100% by Chiral HPLC), + impeccable 1H-NMR, coming with a quantitative elemental analysis. Bulk stock. ship within 1 day.