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Chemical Structure : AMG-458
CAS No.: 913376-83-7
Catalog No.: PC-36035Not For Human Use, Lab Use Only.
AMG-458 (AMG458) is a potent, selective, orally bioavailable c-Met inhibitor with Ki of 1.2 nM (human c-Met).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $488 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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AMG-458 (AMG458) is a potent, selective, orally bioavailable c-Met inhibitor with Ki of 1.2 nM (human c-Met).
AMG-458 also potently binds to mutant c-Met (H1094R), c-Met (V1092I) and c-Met (D1228H) with Ki values of 0.5-2.2 nM.
AMG-458 inhibits HGF-mediated c-Met phosphorylation in PC3 and CT26 cells with IC50 of 60 and 120 nM, abrogates the constitutive phosphorylation of c-Met in H441 cells.
AMG-458 significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models.
| M.Wt | 539.592 | |
| Formula | C30H29N5O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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 |
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1. Liu L, et al. J Med Chem. 2008 Jul 10;51(13):3688-91.
2. Tiedt R, et al. Cancer Res. 2011 Aug 1;71(15):5255-64.
3. van den Heuvel CNAM, et al. Mol Cancer Res. 2017 Nov;15(11):1587-1597.
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