IACS-010759

IACS-010759 is an orally bioavailable inhibitor of complex I of the mitochondrial electron transport chain. It inhibits the ubiquinone reduction activity of isolated murine mitochondrial complex I when used at a concentration of 60 nM. IACS-010759 (100 nM) reduces basal and spare respiratory capacities and increases glycolytic flux in primary chronic lymphocytic leukemia (CLL) cells. It also induces apoptosis in CLL cells grown under low glucose conditions or when administered in combination with 2-deoxy-D-glucose (Cay-14325). IACS-010759 (5 and 10 mg/ml) induces tumor regression in a glycolysis-deficient NB1 mouse xenograft model.Formal Name: 4-(methylsulfonyl)-1-[3-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-1,2,4-triazol-1-yl]methyl]phenyl]-piperidine. CAS Number: 1570496-34-2. Molecular Formula: C25H25F3N6O4S. Formula Weight: 562.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.1 mg/ml, DMSO: 0.2 mg/ml, Ethanol: Slightly soluble. lambdamax: 244 nm. SMILES: CS(C1CCN(C2=CC=CC(CN3C(C)=NC(C4=NC(C5=CC=C(OC(F)(F)F)C=C5)=NO4)=N3)=C2)CC1)(=O)=O. InChi Code: InChI=1S/C25H25F3N6O4S/c1-16-29-23(24-30-22(32-38-24)18-6-8-20(9-7-18)37-25(26,27)28)31-34(16)15-17-4-3-5-19(14-17)33-12-10-21(11-13-33)39(2,35)36/h3-9,14,21H,10-13,15H2,1-2H3. InChi Key: HWJWNWZJUYCGKV-UHFFFAOYSA-N.