FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo[1].
FT113 shows anti-proliferative activity against PC3 and MV-411 cells with IC50s of 47 and 26 nM, respectively[1].
FT113 (5 mg/kg, p.o.) exhibits potent oral bioavailability of 95% and 84% in mice and rats, respectively[1].FT113 (5, 25, or 50 mg/kg, p.o., twice daily for 16 days) increases malonyl-CoA concentration in tumors, inhibits tumor growth in a dose-dependent manner in mice[1].
[1]. Martin MW, et al. Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN). Bioorg Med Chem Lett. 2019 Apr 15;29(8):1001-1006.