MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC 50 s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1 , respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity.