PF-04217903

PF-04217903 is an inhibitor of c-Met (Ki = 4.8 nM). It is greater than 1,000-fold selective for c-Met over a panel of 150 kinases. PF-04217903 inhibits the proliferation of and induces apoptosis in GTL-16 gastric carcinoma cells (IC50s = 12 and 31 nM, respectively) as well as inhibits migration of NCI H441 lung cancer cells induced by hepatocyte growth factor (HGF, IC50 = 11 nM). It reduces tumor growth in a GTL-16 mouse xenograft model when administered at doses ranging from 1 to 30 mg/kg.Formal Name: 4-[1-(6-quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol. CAS Number: 956905-27-4. Molecular Formula: C19H16N8O. Formula Weight: 372.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 2 mg/ml, DMSO:PBS (pH 7.2)(1:8): 0.1 mg/ml. lambdamax: 226, 315, 346 nm. SMILES: OCCN(N=C1)C=C1C2=CN=C3C(N(CC4=CC=C5C(C=CC=N5)=C4)N=N3)=N2. InChi Code: InChI=1S/C19H16N8O/c28-7-6-26-12-15(9-22-26)17-10-21-18-19(23-17)27(25-24-18)11-13-3-4-16-14(8-13)2-1-5-20-16/h1-5,8-10,12,28H,6-7,11H2. InChi Key: PDMUGYOXRHVNMO-UHFFFAOYSA-N.