FT113

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]. IC50 & Target: IC50: 213 nM (FASN), 90 nM (FASN, in BT474 cell)^[1] In Vitro: FT113 shows anti-proliferative activity against PC3 and MV-411 cells with IC₅₀s of 47 and 26 nM, respectively^[1]. In Vivo: 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].