Description: CCT128930 is a novel, potent, ATP-competitive and selective pyrrolopyrimidine-based inhibitor of Akt2 (IC50 = 6 nM in a cell-free assay) with potential anticancer activity. It showed 28-fold greater selectivity for Akt2 over the closely related PKA kinases. CCT128930 was discovered through fragment- and structure-based drug design approaches. CCT128930 exhibited marked antiproliferative activity and inhibited the phosphorylation of a range of AKT substrates in multiple tumor cell lines in vitro, consistent with AKT inhibition. In conclusion, CCT128930 is a novel, potent and selective AKT inhibitor
that blocks AKT activity in vitro and in vivo and induces marked
antitumor responses.
References: Mol Cancer Ther. 2011 Feb;10(2):360-71.