Cas No.: | 913376-83-7 |
Chemical Name: | 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 |
SMILES: | COC1C=CC2=C(OC3C=CC(NC(C4=C(C)N(CC(O)(C)C)N(C5C=CC=CC=5)C4=O)=O)=NC=3)C=CN=C2C=1 |
Formula: | C30H29N5O5 |
M.Wt: | 539.592 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | AMG-458 (AMG458) is a potent, selective, orally bioavailable c-Met inhibitor with Ki of 1.2 nM (human c-Met); also potently binds to mutant c-Met (H1094R), c-Met (V1092I) and c-Met (D1228H) with Ki values of 0.5-2.2 nM; 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; significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models. |