LY2801653

LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM). It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM). LY2801653 (0.01-10 µM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.Formal Name: N-[3-fluoro-4-[[1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl]oxy]phenyl]-1-(4-fluorophenyl)-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarboxamide. CAS Number: 1206799-15-6. Synonyms: Merestinib. Molecular Formula: C30H22F2N6O3. Formula Weight: 552.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 237, 337 nm. SMILES: FC1=CC=C(N2C(C)=CC=C(C(NC3=CC=C(OC4=C(C5=CNN=C5)C=C(N(C)N=C6)C6=C4)C(F)=C3)=O)C2=O)C=C1. InChi Code: InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39). InChi Key: QHADVLVFMKEIIP-UHFFFAOYSA-N.