NVP-BKM120 is a potent inhibitor of class I PI3K isoforms; potently blocks both p110α (IC₅₀ = 52 nM) and p110β (IC₅₀ = 166 nM) in vitro. It is much less effective against the class III PI3K Vps34 and mammalian target of rapamycin (mTOR) and has no effect on PI4Kβ and several other kinases. NVP-BKM120 prevents the growth of assorted cancer cell lines when used at 5 μM and inhibits tumor growth in vivo.