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 Ki of 0.42 nM, 0.6 nM, 0.47 nM and 1.7 nM, respectively. In T47D and BT474 cancer cells, GSK1059615 inhibits the phosphorylation of Akt at S473, with IC50 of 40 nM.
In Vivo: GSK1059615 (25 mg/kg) effectively inhibits tumor growth in xenograft mice models of BT474 or HCC1954 breast cancer cells.
Related Products:
PKI-402; Voxtalisib; Pilaralisib; PI-3065; VS-5584; PIK-294; AZD6482; AZD8186; CUDC-907; AZD8835; AMG319; Buparlisib hydrochloride; Umbralisib; PIK-III; VPS34-IN1; VPS34 inhibitor 1; Wortmannin