NVP-BKM120

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 of kinases (IC50s = >10,000 nM). NVP-BKM120 inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells being more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively). It halts the cell cycle in the G2/M phase in both p53 wild-type and p53 mutant/deleted glioma cells, but p53 mutant/deleted cells reenter the cell cycle, progress into mitosis, and die via mitotic catastrophic cell death. NVP-BKM120 (1-5 mg/kg) crosses the blood brain barrier and selectively decreases phosphorylation of the PI3K target protein Akt. It increases survival in a U87 glioma mouse xenograft intracranial tumor model when administered orally at doses of 20 and 40 mg/kg once per week.Formal Name: 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-2-pyridinamine. CAS Number: 944396-07-0. Synonyms: Buparlisib. Molecular Formula: C18H21F3N6O2. Formula Weight: 410.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12 mg/ml, DMSO: 14 mg/ml, Ethanol: 17 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 232, 254, 318 nm. SMILES: NC(N=C1)=CC(C(F)(F)F)=C1C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2. InChi Code: InChI=1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23). InChi Key: CWHUFRVAEUJCEF-UHFFFAOYSA-N.