BAY-1125976 is a potent and highly selective, allosteric AKT1/2 inhibitor with IC50 of 5.2/18 nM at 10 uM ATP.
BAY-1125976 binds to active AKT1 with Kd of 2.7 nM and inactive AKT1 with Kd of 1.3 nM.
BAY-1125976 displays >86-fold less potent against AKT3; inhibits the phosphorylation of AKT1 at T308 and S473 (IC50=0.9 and 1.1 nM, respectively), PRAS40 at T246 and 4EBP1 at T70.
BAY-1125976 targets tumors displaying PI3K/AKT/mTOR pathway activation, inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors.
BAY-1125976 exhibits strong in vivo patient-derived xenograft models.
