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PI3 kinase inhibitor BEZ 235, 5 mg  

PI3 kinase inhibitor BEZ 235, 5 mg

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

Synonyms: NVP-BEZ235, Dactolisib
BEZ 235 is an orally active PI3 kinase (Phosphatidylinositol 3-kinase) inhibitor.

More details

PKI-BEZ235-005

Availability: within 3 days

97,50 €

Background: BEZ 235 is an orally active PI3K kinase inhibitor; Dual inhibition of p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM. BEZ235 showed high target specificity and demonstrated antiproliferative activity against tumor cell lines in animal models of cancer.

Chemical formula: C30H23N5O
Molecular weight:469.54 g/mol
Purity: 99 %
Appearance: Off-white Solid
Solubility: Moderately soluble in DMSO
CAS Number: 915019-65-7

Manufacturer:  Axon Medchem BV

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.  

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.

Toledo LI, et al. Nat Struct Mol Biol, 2011, 18(6), 721-727.

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