GNE-617

GNE-617 is a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt, IC50 = 5 nM). It has antiproliferative activity in U251 glioblastoma, HT-1080 fibrosarcoma, PC3 prostate, MiaPaCa2 pancreatic, and HCT116 colon cancer cell lines (IC50s = 1.8, 2.1, 2.7, 7.4, and 2.0 nM, respectively). In a U251 mouse xenograft model, GNE-617 (25 mg/kg once per day) led to rapid tumor regression.Formal Name: N-[[4-[(3,5-difluorophenyl)sulfonyl]phenyl]methyl]-imidazo[1,2-a]pyridine-6-carboxamide. CAS Number: 1362154-70-8. Molecular Formula: C21H15F2N3O3S. Formula Weight: 427.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 238 nm. SMILES: FC1=CC(S(C2=CC=C(CNC(C(C=C3)=CN4C3=NC=C4)=O)C=C2)(=O)=O)=CC(F)=C1. InChi Code: InChI=1S/C21H15F2N3O3S/c22-16-9-17(23)11-19(10-16)30(28,29)18-4-1-14(2-5-18)12-25-21(27)15-3-6-20-24-7-8-26(20)13-15/h1-11,13H,12H2,(H,25,27). InChi Key: XRDVXQQZLHVEQZ-UHFFFAOYSA-N.