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BEZ235 inhibits PI3K and mTORC1/2, exhibiting anticancer chemotherapeutic activity. In nasopharyngeal cancer cells, BEZ235 induces G1 phase cell cycle arrest and apoptosis; in similar animal models of nasopharyngeal or cholangiocarcinoma, this compound inhibits tumor growth. BEZ235 also induces apoptosis in hepatocellular carcinoma cells, also potentially inducing autophagy.
| Cas No. | 915019-65-7 |
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| Purity | ≥98% |
| Formula | C30H23N5O |
| Formula Wt. | 469.54 |
| IUPAC Name | 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile |
| Synonym | NVP-BEZ235, Dactolisib |
| Solubility | DMF 18 mg/mL warmed (38.33 mM) DMSO 0.01 mg/mL (0.02 mM) Water Insoluble |
| Appearance | White Crystal Powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet | |
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Ma BB, Lui VW, Hui CW, et al. Preclinical evaluation of the mTOR-PI3K inhibitor BEZ235 in nasopharyngeal cancer models. Cancer Lett. 2014 Feb 1;343(1):24-32. PMID: 24041865.
Yothaisong S, Dokduang H, Techasen A, et al. Increased activation of PI3K/AKT signaling pathway is associated with cholangiocarcinoma metastasis and PI3K/mTOR inhibition presents a possible therapeutic strategy. Tumour Biol. 2013 Dec;34(6):3637-48. PMID: 23832540.
Chang Z, Shi G, Jin J, et al. Dual PI3K/mTOR inhibitor NVP-BEZ235-induced apoptosis of hepatocellular carcinoma cell lines is enhanced by inhibitors of autophagy. Int J Mol Med. 2013 Jun;31(6):1449-56. PMID: 23588698.