AMG 1

AMG 1 is an inhibitor of c-Met and Ron (IC50s = 4 and 9 nM, respectively). It is selective for c-Met and Ron over seven tyrosine and serine/threonine kinases (IC50s = 160 to 1,900 nM). AMG 1 decreases the levels of phosphorylated MET, ERK1/2, and Akt in HT-29 colon and BxPC-3 pancreatic cancer cells, as well as reduces migration in a wound-healing assay using NIH3T3/TPR-Met fibroblasts, in a concentration-dependent manner. It reduces tumor volume in a U87 glioma mouse xenograft model when administered at a dose of 30 mg/kg twice per day. AMG 1 increases bone volume and bone regrowth area in a mouse model of calvarial defect when administered at a dose of 50 µg in an absorbable collagen sponge.Formal Name: N-[3-fluoro-4-[(7-methoxy-4-quinolinyl)oxy]phenyl]-2,3-dihydro-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-1H-pyrazole-4-carboxamide. CAS Number: 913376-84-8. Synonyms: KIN001-237, KIN237, RON-IN-1, RON Inhibitor 1, SYN1143. Molecular Formula: C31H29FN4O5. Formula Weight: 556.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml. SMILES: OC(C)(C)CN(C(C)=C1C(NC2=CC(F)=C(OC3=C(C=CC(OC)=C4)C4=NC=C3)C=C2)=O)N(C5=CC=CC=C5)C1=O. InChi Code: InChI=1S/C31H29FN4O5/c1-19-28(30(38)36(21-8-6-5-7-9-21)35(19)18-31(2,3)39)29(37)34-20-10-13-27(24(32)16-20)41-26-14-15-33-25-17-22(40-4)11-12-23(25)26/h5-17,39H,18H2,1-4H3,(H,34,37). InChi Key: UYMSIPINLJNNOU-UHFFFAOYSA-N.