As a novel and dual inhibitor, GSK1059615 can inhibit PI3Kalpha, PI3Kbeta, PI3Kdelta, PI3Kgamma and mTOR with IC50 of 0.4 nM, 0.6 nM, 2 nM, 5 nM and 12 nM. In T47D and BT474 cancer cells, GSK1059615 inhibits the phosphorylation of Akt at S473, with IC50 of 40 nM. [4]
In vivo
In xenograft mice models of BT474 or HCC1954 breast cancer cells, GSK1059615 (25 mg/kg) shows strong inhibition to tumor growth.