NVP-BAG956 (BAG956) is a potent, dual PDK-1/PI3K inhibitor with IC50 of 245/56/446/35/117 nM for PDK1/p110α/p110β/p110δ/p110γ, respectively.
NVP-BAG956 inhibits p-T308-PKB U87MG cells with IC50 of 45 nM in ELISA assays, shows anti-proliferative activity with EC50 of 143 nM.
NVP-BAG956 blocks AKT phosphorylation induced by BCR-ABL–, and induces apoptosis of BCR-ABL–expressing cell lines and patient bone marrow cells at concentrations that also inhibit PI3K signaling.
NVP-BAG956 demonstrates against BCR-ABL expressing cells both in vitro and in vivo, BAG956 is effective against mutant FLT3-expressing cell lines and AML patient bone marrow cells.
