GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays. It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by activated Akt, halting cell cycle progression and reducing cell viability. In multiple tumor xenograft models, oral administration of GDC-0068 at 100 mg/kg/day can lead to delayed tumor growth and regression.
