NVP-BEZ235（PI3K/mTOR inhibitor

Biological Activity

NVP-BEZ235, an imidazo[4,5-c]quinoline derivative, is a ATP-competitive, orally available and potent dual pan-PI3K/mTOR inhibitor, which effectively blocks the dysfunctional activation of the PI3K pathway in cellular and in vivo settings, and displays diseases stasis in relevant in vivo models of human cancer as well as enhances the antitumor activity of other cancer agents. Kinase assays show that the molecule inhibits the activity of class I PI3K at low nanomolar potency including the E545K or H1047R mutant forms of PI3Kα, but poorly suppresses (IC₅₀ >10 μM) a representative panel of protein kinases, including Akt and PDK1. NVP-BEZ235 directly inhibits both mTORC1 and mTORC2 with an IC₅₀ of 20.7 nM ^[1]. Through its effect on PI3K/mTOR axis, NVP-BEZ235 strongly inhibits VEGF-induced angiogenesis in vivo ^[2], and causes inhibition of cell proliferation and tumor growth in cancer cells with both wild-type and mutated p110α ^[3]. NVP-BEZ235 abrogates phosphatidylinositol 3-kinase (PI3K)-induced lapatinib resistance ^[4].

Chemical Properties

Cas No.: 915019-65-7	M. Wt.: 469.54
Formula: C30H23N5O	Purity: >99%
Synonym: BEZ235
Chemical Name:2-methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1yl)phenyl)propanenitrile
Appearance: White to off-white solid
Solubility: Soluble in DMSO approximately at 1 mg/ml with warming. Very poorly soluble in ethanol and water.
Storage：Store solid at -20 ºC for the stability of 2 years, protect from light.