GNE-493 是选择性的PI3K/mTOR抑制剂，能够抑制 PI3Kα (IC50:3.4 nM)，PI3Kβ (IC50:12 nM)，PI3Kδ (IC50:16 nM)，PI3Kγ (IC50:16 nM) 和 mTOR (IC50:32 nM)。

GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR,respectively.

GNE-493 is examined in the human MCF7.1 breast cancer xenograft model that harbors a PI3Kα activating mutation. Mice bearing xenografts are dosed orally once daily with 10 mg/kg of GNE-493 for 21 continuous days. Similar to observations made in the PC3 prostate cancer xenograft model, 10 mg/kg of GNE-493 results in 73% tumor growth inhibition at day 21 when compared to vehicle control animals. When achieving comparable levels of drug exposure, GNE-493 shows a similar suppression of the PI3K pathway and consequently, a similar efficacy profile against MCF7.1 breast tumors

1033735-94-2

C17H20N6O2S

372.45

DMSO:45 mg/mL (120.82 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years