tcsc3359 GNE-477

GNE-477 is a potent and efficacious dual PI3K (IC₅₀=4 nM)/mTOR(K_i=21 nM) inhibitor.

IC50 & Target: IC50: 4 nM (PI3Kα)^[1]


Ki: 21 nM (mTOR)^[1]

In Vitro: GNE-477 (Compound 8) has improved potency in the MCF7.1 cell proliferation assay with an EC₅₀ of 143 nM^[1].

In Vivo: GNE-477 also exhibits stasis in a PC3 tumor growth inhibition study. In an experiment evaluating the tumor growth inhibition of a PC3 tumor xenograft over 14 days, stasis is achieved at a 20 mg/kg QD dose and significant inhibition is observed with doses as low as 1 mg/kg QD. GNE-477 is generally well tolerated during this study as demonstrated by acceptable levels of weight loss comparable to that observed with the animals in the vehicle cohort^[1].