BX-912 is an aminopyrimidine-based, ATP-competitive inhibitor of PDK1 at an IC50 of 12 nM. In a panel of relevant serine-threonine and receptor-tyrosine kinases, BX-912 showed at least 20-fold selectivity with the exception of 9-fold selectivity (110 nM) for PKA. In a panel of cell lines, BX-912 potently inhibits growth of PC-3 cells in soft agar at an IC50 of 320 nM. (1)