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AMG-458 is an inhibitor of c-MET that exhibits anticancer chemotherapeutic activity. AMG-458 enhances the radiosensitivity of lung adenocarcinoma cells, decreasing activation of Akt and ERK and inducing apoptosis. In vivo, this compound inhibits the growth of glioblastoma tumors.
| Cas No. | 913376-83-7 |
|---|---|
| Purity | ≥98% |
| Formula | C30H29N5O5 |
| Formula Wt. | 539.58 |
| IUPAC Name | 1-(2-hydroxy-2-methylpropyl)-N-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide |
| Synonym | AMG458 |
| Solubility | DMSO 21 mg/mL (38.91 mM) Water Insoluble Ethanol Insoluble |
| Appearance | White Crystal Powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Li B, Torossian A, Sun Y, et al. Higher levels of c-Met expression and phosphorylation identify cell lines with increased sensitivity to AMG-458, a novel selective c-Met inhibitor with radiosensitizing effects. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e525-31. PMID: 22836051.
Liu L, Siegmund A, Xi N, et al. Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem. 2008 Jul 10;51(13):3688-91. PMID: 18553959.
