NVP-TNKS656

NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2, IC50 = 6 nM). It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/beta-catenin target gene, in MMTV-Wnt1 tumor bearing mice.Formal Name: N-(cyclopropylmethyl)-4-(4-methoxybenzoyl)-N-[(3,5,7,8-tetrahydro-4-oxo-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl]-1-piperidineacetamide. CAS Number: 1419949-20-4. Molecular Formula: C27H34N4O5. Formula Weight: 494.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 279 nm. SMILES: O=C(N=C(CN(CC1CC1)C(CN2CCC(C(C3=CC=C(OC)C=C3)=O)CC2)=O)N4)C5=C4CCOC5. InChi Code: InChI=1S/C27H34N4O5/c1-35-21-6-4-19(5-7-21)26(33)20-8-11-30(12-9-20)16-25(32)31(14-18-2-3-18)15-24-28-23-10-13-36-17-22(23)27(34)29-24/h4-7,18,20H,2-3,8-17H2,1H3,(H,28,29,34). InChi Key: DYGBNAYFDZEYBA-UHFFFAOYSA-N.