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M2912 is an inhibitor of tankyrase 1 (TNKS1) and TNKS2 (IC50s = 0.6 and 0.9 nM, respectively).1 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.
WARNING This product is not for human or veterinary use.
1. Optimization of a screening hit toward M2912, an oral tankyrase inhibitor with antitumor activity in colorectal cancer models. J. Med. Chem. 64(14), 10371-10392 (2021).