AZD8835 is a selective, oral inhibitor of PI3K isoforms and with the following activity in enzymatic assays: PI3K C IC50 = 6nM (equipotent vs wt and E545K / H1047R mutants); PI3K C IC50 = 6nM; PI3K C IC50 = 90nM; PI3K C IC50 = 431nM. Inhibition of signalling in cells (pAKT endpoint): PI3K C IC50= 57nM; PI3K C IC50= 49nM; PI3K C IC50= 3.6M; PI3K - IC50= 532nM
Description: Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.