BEZ235
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.
References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18843777
Cas No. |
915019-65-7 |
---|---|
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 |
Appearance |
White Crystal Powder |
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.