Biological Activity:

Orally active PI3K tyrosine kinase inhibitor; Dual PI3K/mTOR inhibition; BEZ235 showed high target specificity and demonstrated antiproliferative activity against tumor cell lines in animal models of cancer.

References:

JC Verheijen, A Zask. Phosphatidylinositol 3-kinase (PI3K) inhibitors as anticancer drugs. Drugs Fut 2007, 32(6), 537.

SM Maira et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther 2008, 7(7), 1851–1863.

R Marone et al. Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors. Mol. Cancer Res. 2009, 7(4), 601-613.

SM Maria, P Furet and F Stauffer. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway. Future Med. Chem. 2009, 1(1), 137-155.

SM Brachmann et al. Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells. PNAS, 2009, 106 (52), 22299-22304.

Chemical Name: 2-Methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile