NVP-BEZ235 is a dual inhibitor of class I PI3Ks (IC50s = 4, 75, 7, and 5 nM, for p110alpha, - beta, -delta, and -gamma, respectively) and mTOR (IC50 = 20 nM). It is selective for these enzymes over a panel of kinases (IC50s = >10 µM for all). NVP-BEZ235 (0.1 or 1 µM) inhibits proliferation of, and induces apoptosis...

White to off-white solid. Soluble in dimethylformamide (~10mg/ml). Sligthly soluble in DMSO or chloroform (~1mg/ml). Warming and sonication might be necessary. Insoluble in water. Potent dual ATP-competitive pan class I PI3K and mTOR inhibitor (p110alpha/gamma/delta/beta and mTOR(p70S6K) with IC50 of 4nM, 5nM, 7nM,...

BEZ235 inhibits PI3K and mTORC1/2, exhibiting anticancer chemotherapeutic activity. In nasopharyngeal cancer cells, BEZ235 induces G1 phase cell cycle arrest and apoptosis, in similar animal models of nasopharyngeal or cholangiocarcinoma, this compound inhibits tumor growth. BEZ235 also induces apoptosis in...

Description: Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110alpha, 5 nM for p110gamma, 7 nM for p110delta, 75 nM for p110beta, and 20.7 nM for mTOR. Target: ATM/ATR, Autophagy, PI3K, mTOR. Smiles:...