G007-LK

G007-LK is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 46 and 25 nM, respectively). It is selective for TNKS1 and TNKS2 over a panel of 90 kinases, 16 phosphatases, and 73 G protein-coupled receptors (GPCRs) when used at a concentration of 10 µM. G007-LK inhibits colony formation of COLO 320 DM and SW403 colorectal cancer cell lines when used at a concentration of 200 µM, as well as human hepatocellular carcinoma (HCC) cells in a dose-dependent manner. It increases expression of intestinal differentiation markers in COLO 320 DM and HCT15 cells when used at a concentration of 100 nM. G007-LK inhibits Wnt3A-induced signaling in human HEK293 and mouse 10T1/2 cells. G007-LK (20 mg/kg, i.p., twice daily) also inhibits tumor growth in COLO 320 DM and SW403 mouse xenograft models, however, it leads to intestinal toxicity when administered at a dose of 30 mg/kg twice daily, leading to moribundity and death.Formal Name: 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-benzonitrile. CAS Number: 1380672-07-0. Synonyms: Tankyrase 1/2 Inhibitor VI. Molecular Formula: C25H16ClN7O3S. Formula Weight: 530.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 25 mg/ml. lambdamax: 330 nm. SMILES: ClC(C=CC=C1)=C1N2C(/C=C/C3=NN=C(C4=CC=C(C#N)C=C4)O3)=NN=C2C5=NC=C(S(C)(=O)=O)C=C5. InChi Code: InChI=1S/C25H16ClN7O3S/c1-37(34,35)18-10-11-20(28-15-18)24-31-29-22(33(24)21-5-3-2-4-19(21)26)12-13-23-30-32-25(36-23)17-8-6-16(14-27)7-9-17/h2-13,15H,1H3/b13-12+. InChi Key: HIWVLHPKZNBSBE-OUKQBFOZSA-N.