NVP-BKM120 is a potent, selective, orally bioavailable Class I PI3 Kinase Inhibitor for treating Cancer.BKM120 is a potent and cell permeable inhibitor of the PI 3-kinase family. Specifically inhibits p110α, p110β, p110γ and p110δ with IC50 of 52 nM, 166 nM, 262 nM and 116 nM, respectively.
Phosphatidylinositol 3-kinases (PI3K) belong to a family of lipid kinases that is involved in many types of cancer. NVP-BKM120 is an orally bioavailable inhibitor of class I PI3K isoforms, potently blocking, in vitro, both p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM).It much less effectively inhibits the class III PI3K Vps34 and mammalian target of rapamycin and has no effect on PI4Kβ and several other kinases.2 NVP-BKM120 prevents the growth of assorted cancer cell lines when used at 5 μM and inhibits tumor growth in vivo. It can be particularly effective against certain types of cancer when combined with other modulators.