IPI-9119 是一种具有口服活性、选择性和不可逆的 FASN 抑制剂 (IC50 = 0.3 nM)。

IPI-9119 is an orally active, selective and irreversible FASN inhibitor (IC50 = 0.3 nM).

IPI-9119 (0.05, 0.1, 0.25, 0.5, 5 μM; 6 days) inhibits AR-FL and AR-V7 protein expression. IPI-9119 (0.1, 0.5 μM; 6 days) inhibits cell growth and induces cell cycle arrest and apoptosis[1]. IPI-9119 inhibits FASN in cellular occupancy assays (IC50~10nM) and shows more than 400-fold selectivity against several additional serine hydrolases[2].

IPI-9119 inhibits tumor growth of castration-resistant prostate cancer in xenografts mouse models[1].

1346564-56-4

C24H19F2N5O5

495.43

DMSO:100 mg/mL (201.84 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years