tcsc0187 GSK1059615

GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC₅₀ of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.

IC50 & Target: IC50: 0.4 nM (PI3Kα), 0.6 nM (PI3Kβ), 2 nM (PI3Kδ), 5 nM (PI3Kγ), 12 nM (mTOR)

In Vitro: GSK1059615 inhibits PI3Kα, β, γ and δ, with K_i of 0.42 nM, 0.6 nM, 0.47 nM and 1.7 nM, respectively^[1]. In T47D and BT474 cancer cells, GSK1059615 inhibits the phosphorylation of Akt at S473, with IC₅₀ of 40 nM^[2].

In Vivo: GSK1059615 (25 mg/kg) effectively inhibits tumor growth in xenograft mice models of BT474 or HCC1954 breast cancer cells^[1].