GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with Ki/IC50 of 0.89/5.2 nM, respectively. GSK2636771 displays 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms. GSK2636771 causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells. GSK2636771 decreases AKT phosphorylation in prostate and breast cancer cell lines, suppresses cell and tumor growth in vivo.
