BEZ235 [ Discontinued ]
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BEZ235, an imidazoquinoline derivative, is a dual ATP-competitive inhibitor of phosphatidylinositol 3 kinase (PI3K) and the mammalian target of rapamycin (mTOR).
PI3K, an important intracellular mediator, regulates multiple cellular functions including cell growth and survival. PI3K activates a number of downstream targets including the serine/threonine kinase Akt that activates mTOR, the master negative regulator of autophagy.
By inhibiting mTOR activity, BEZ235 induces autophagy and promotes cells survival . In contrast, the combination of BEZ235 with autophagy inhibitors, such as 3-methyladenine, inhibits cell growth and induces apoptosis [2, 3].
Furthermore, in experimental models, BEZ235 blocks angiogenesis through the inhibition of PI3K .
1. Chang Z. et al., 2013. Dual PI3K/mTOR inhibitor NVP-BEZ235-induced apoptosis of hepatocellular carcinoma cell lines is enhanced by inhibitors of autophagy. Int J Mol Med. 31(6):1449-56.
2. Roper J. et al., 2011. The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer. PLoS One. 6(9):e25132.
3. Bhatt AP. et al., 2010. Dual inhibition of PI3K and mTOR inhibits autocrine and paracrine proliferative loops in PI3K/Akt/mTOR-addicted lymphomas. Blood. 115(22):4455-63.
4. Schnell CR. et al., 2008. Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging. Cancer Res. 68(16):6598-607.
Solubility: 1 mg/ml (2.13 mM) in DMSO.
Synonym: NVP-BEZ235, Dactolisib.
CAS number: 915019-65-7.
Molecular weight: 469.55.
Working Concentration: 1-500 nM.Back to the top
BEZ235 is provided as a solid.
- 50 mg BEZ235
BEZ235 is shipped at room temperature.
Store at -20 °C.Back to the top