AT-13148

AT13148 is a potent, ATP-competitive multi-AGC kinase inhibitor that displays antitumor activity. AT13148 blocks AKT, p70S6K, PKA, ROCK, and SGK substrate phosphorylation inducing concentration dependent apoptosis in cancer cells. It also shows anti-tumor efficacy in HER2-positive, PIK3CA-mutant BT474 breast, PTEN-deficient PC3 human prostate cancer and PTEN deficient MES-SA uterine tumor in xenografts. Gene expression studies shows that AT13148 has a predominant effect on apoptosis genes.