AMG 458

AMG 458 is an inhibitor of c-Met (Kis = 1.2, 1.1, 2.2, 4.1, 0.5, and 4.5 nM for wild-type c-Met, c-MetV1092I, c-MetD1228H, c-MetM1250T, c-MetH1094R, and c-MetY1230H, respectively). It inhibits c-Met phosphorylation in PC3 and CT26 cells (IC50s = 60 and 120 nM, respectively). AMG 458 (30 and 100 mg/kg) reduces tumor volume in NIH3T3 and U87MG mouse xenograft models.Formal Name: 2,3-dihydro-1-(2-hydroxy-2-methylpropyl)-N-[5-[(7-methoxy-4-quinolinyl)oxy]-2-pyridinyl]-5-methyl-3-oxo-2-phenyl-1H-pyrazole-4-carboxamide. CAS Number: 913376-83-7. Molecular Formula: C30H29N5O5. Formula Weight: 539.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 234, 301 nm. SMILES: O=C(C1=C(C)N(CC(C)(O)C)N(C2=CC=CC=C2)C1=O)NC3=CC=C(C=N3)OC4=CC=NC5=C4C=CC(OC)=C5. InChi Code: InChI=1S/C30H29N5O5/c1-19-27(29(37)35(20-8-6-5-7-9-20)34(19)18-30(2,3)38)28(36)33-26-13-11-22(17-32-26)40-25-14-15-31-24-16-21(39-4)10-12-23(24)25/h5-17,38H,18H2,1-4H3,(H,32,33,36). InChi Key: GLBZSOQDAOLMGC-UHFFFAOYSA-N.