NPS 1034

NPS 1034 is a dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM), receptors for hepatocyte growth factor and vitamin K-dependent proteins, respectively. It synergistically inhibits cell proliferation when used in combination with gefitinib (Cay-13166) or erlotinib (Cay-10483) in NSCLC cells with acquired resistance to EGFR receptor tyrosine kinase inhibitors. NPS 1034 inhibits autophosphorylation of numerous constitutively active mutant forms of MET (IC50s <25 nM) and inhibits the invasion and migration of MET mutant-transfected cells. It also inhibits growth of MKN45 xenograft tumors in mice treated orally with 30 mg/kg NPS 1034 for 25 days.Formal Name: 2-(4-fluorophenyl)-N-[3-fluoro-4-[(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,3-dihydro-1,5-dimethyl-3-oxo-1H-pyrazole-4-carboxamide. CAS Number: 1221713-92-3. Molecular Formula: C31H23F2N5O3. Formula Weight: 551.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml, Ethanol: 1 mg/ml. lambdamax: 286 nm. SMILES: FC(C=C(NC(C1=C(C)N(C)N(C2=CC=C(F)C=C2)C1=O)=O)C=C3)=C3OC4=C5C(NC=C5C6=CC=CC=C6)=NC=C4. InChi Code: InChI=1S/C31H23F2N5O3/c1-18-27(31(40)38(37(18)2)22-11-8-20(32)9-12-22)30(39)36-21-10-13-25(24(33)16-21)41-26-14-15-34-29-28(26)23(17-35-29)19-6-4-3-5-7-19/h3-17H,1-2H3,(H,34,35)(H,36,39). InChi Key: RGAZVGZUBCFHRJ-UHFFFAOYSA-N.