M2912

M2912 is an inhibitor of tankyrase 1 (TNKS1) and TNKS2 (IC50s = 0.6 and 0.9 nM, respectively). It is selective for TNKS1 and TNKS2 over poly(ADP-ribose) polymerase 1 (PARP1, IC50 = 928 nM). M2912 increases the levels of Axin2 (EC50 = 17 nM) and reduces Wnt reporter activity in DLD-1 cells. It reduces the growth of a variety of colorectal cancer cells in vitro at 0.01-10 µM and reduces tumor volume in a COLO 320 mouse xenograft model at 20 mg/kg.. SMILES: CC(O)(C1=CC=C(C(N2)=CN3C(C)=CC=C3C2=O)C=C1)C. InChi Code: InChI=1S/C17H18N2O2/c1-11-4-9-15-16(20)18-14(10-19(11)15)12-5-7-13(8-6-12)17(2,3)21/h4-10,21H,1-3H3,(H,18,20). InChi Key: MPXAEYSGFKRDQM-UHFFFAOYSA-N