Product Name: NVP-BEZ 235
Synonyms: 2-methyl-2-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)propanenitrile;2-Methyl-2-[3-Methyl-2-oxo-8-(3-quinolinyl)-1-iMidazo[4,5-c]quinolinyl]propanenitrile;4-[2,3-Dihydro-3-Methyl-2-oxo-8-(quinolin-3-yl)-1H-iMidazo[4,5-c]quinolin-1-yl]-alpha,alpha-diMethylbenzeneacetonitrile;BEZ-235;4-[2,3-Dihydro-3-Methyl-2-oxo-8-(3-quinolinyl)-1H-iMidazo[4,5-c]quinolin-1-yl]-α,α-diMethyl-benzeneacetonitrile;NVP-BEZ235(BEZ235);BEZ235 (NVP-BEZ235, Dactolisib);2-Methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)phenyl
CAS: 915019-65-7
MF: C30H23N5O
MW: 469.54
EINECS: 1312995-182-4
Product Categories: Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators;api;Inhibitors;Akt;mTOR;PI3K
Melting point 288-289°C
density 1.299
storage temp. Refrigerator
Uses A dual ATP-competitive inhibitor of PI3K and mTOR. p110α, IC50=4 nM; p110β, IC50=75 nM; p110δ, IC50=7 nM; p110γ, IC50=5 nM.
Uses Inhibitor of phosphatidylinositol 3-kinases, P13K and mTOR.
Uses Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies. It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase. Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis. By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.[Cayman Chemical]