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Description
Background Information:
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.
Reference:
1. Z.Q. Du, et al, Preclinical evaluation of AMG 337, a highly selective small molecule MET inhibitor, in hepatocellular carcinoma, Cancer Res, August 1, 2015 75; 5391.
APIM050075: AMG-337
CAS No.: 1173699-31-4.
Molecular Formula: C23H22FN7O3 ? 0.5H2O.
Molecular Weight: 472.5.
Purity: 99.7-100% by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
Additional information
| Ship from Country | USA |
|---|---|
| Size | 10 mg, 100 mg, 200 mg, 5 mg, 50 mg |
