FT113 是一种有效、可口服的脂肪酸合酶 (fatty acid synthase (FASN)) 抑制剂，对全长重组人 FASN 酶的 IC50 值为 213 nM。在 BT474 细胞中，FT113 抑制 FASN 的活性，IC50 值为 90 nM。FT113 具有抗增殖作用，在体内和体外实验中，都具有抗癌作用。
货号:ajcx38666
CAS:1630808-89-7
分子式:C22H20FN3O4
分子量：409.41
溶解度:DMSO : 62.5 mg/mL (152.66 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.