Tankyrase Inhibitors (TNKS) 22 Tankyrase inhibitor

Tankyrase Inhibitors (TNKS) 22 was evaluated for Wnt-pathway specific pharmacological activity in mouse tumor pharmacodynamic (PD) models. Upon once daily oral administration (at 10 and 50 mg/kg) to mice (n=4) bearing human DLD-1 tumors for 3 days, both compounds exhibited statistically significant, dose-dependent axin2 accumulation (2.7-to 3.5-fold) and inhibition of STF (51−58%) at day 3 (24 h after the last dose) .