Description: Buparlisib (BKM120) is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110alpha, p110beta, and p110delta). Target: Apoptosis, PI3K. Smiles: Nc1cc(c(cn1)-c1cc(nc(n1)N1CCOCC1)N1CCOCC1)C(F)(F)F. References: Burger MT, et al. Identification of NVP-BKM120 as...

NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110alpha (IC50 = 52 nM) and p110beta (IC50 = 166 nM). It is selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), the mammalian target of rapamycin (mTOR, IC50 = 2,866 nM), PI4Kbeta (IC50 = >25,000 nM), and a variety...

BKM120 is an inhibitor of PI3K that is currently in clinical trials as a potential treatment for brain metastases of HER2+ breast cancer and other solid tumors. BKM120 exhibits anticancer chemotherapeutic activity, inducing G2/M phase cell cycle arrest, polyploidy, and apoptosis in glioblastoma cells. Additionally,...

Soluble in DMSO or ethanol. NVP-BKM120 is a potent, selective, orally bioavailable Class I PI3Kalpha Inhibitor with IC(50) of 20nM, currently in Phase II clinical trials for the treatment of cancer. It exhibits lower potency against class III and class IV PI3Ks Target: PI3K , Kinase Group: Lipid Kinase ,...