CCT128930 is a potent, selective, ATP-competitive AKT inhibitor with IC50 of 6 nM (AKT2), 28-fold selectivity over the closely related PKA.
CCT128930 also exhibits 20-fold selectivity over p70S6K (IC50=120 nM).
CCT128930 shows growth inhibition for U87MG human glioblastoma cells (IC50=6.3 uM), for LNCaP human prostate cancer cells (IC50=0.35 uM), and for PC3 human prostate cancer cells (IC50=1.9 uM) consistent with AKT pathway blockade.
CCT128930 blocks the phosphorylation of several downstream AKT biomarkers in U87MG tumor xenografts, indicating AKT inhibition in vivo.
CCT128930 demonstrates antitumor activity in U87MG and HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts.
