GNF-6231 shows IC50s of greater than 10 uM on all CYP isoforms tested . GNF-6231 have favorable potency and a PK profile across preclinical species upon oral administration. The reference for orally in MMTV-Wnt1 tumor bearing mice is dosed at 3 mg/kg. GNF-6231 showed very robust dose-related antitumor efficacy. GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.