NVP-BEZ235, BEZ235

For research purposes only

Cat. No BA94673129

Availability - up to 100 mg in stock
- larger amount can be synthesized in 8 weeks

Description of biological activity

NVP-BEZ235 is a dual PI3K/mammalian target of rapamycin (mTOR) inhibitor in gliomas with specificity against several PI3K kinases [2]. The compound suppressed glioma cell proliferation with IC(50) values in the low nanomolar range by specifically inhibiting the activity of target proteins including Akt, S6K1, S6, and 4EBP1 in the PI3K/Akt/mTOR signaling pathway. NVP-BEZ235 treatment of glioma cell lines led to G(1) cell cycle arrest and induced autophagy. It was the first PI3K inhibitor to enter clinical trials and have currently reached phase II in patients with solid tumors.
IC50: 4nM (PI3Kα),75nM (PI3Kβ), 5nM (PI3Kγ), 7nM (PI3Kδ) [3]
Target: PI3K family kinase

Therapeutic area

Glioblastoma, lung, multiple myeloma, non-Hodgkin's lymphoma, pancreas, prostate sarcoma

Biological target category

Phosphoinositide 3-kinase PI3K(s)

TECHNICAL INFORMATION

2-methyl-2-(4-{3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl}-phenyl)-propionitrile Inhibitor of Phosphatidylinositol 3-Kinases (PI3K(s))

IUPAC 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

Chemical Formula: C30H23N5O

CAS Number: 915019-65-7

Molecular Weight: 469.550

Purity: > 98% chemical purity (LCMS)

Solubility: 10 mM in DMSO

1H-NMR spectrum (click to enlarge)

REFERENCES

[1] NOVARTIS AG; NOVARTIS PHARMA GMBH. IMIDAZOQUINOLINES AS LIPID KINASE INHIBITORS WO2006/122806 A2, 2006

[2] Liu TJ et al. NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas. Mol Cancer Ther. 2009 Aug;8(8):2204-10

[3] Ciraolo E, et al. Present and Future of PI3K Pathway Inhibition in Cancer: Perspectives and Limitations. Curr Med Chem. 2011;18(18):2674-85.

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