915019-65-7

溶解度:DMSO

储存条件:-20C 2 years

生物活性

Orally active PI3K tyrosine kinase inhibitor; Dual PI3K/mTOR inhibition; BEZ235 showed high target specificity and demonstrated antiproliferative activity against tumor cell lines in animal models of cancer.

NVP-BEZ235 inhibited the activation of the downstream effectors Akt, S6 ribosomal protein, and 4EBP1 in breast cancer cells. The antiproliferative activity of NVP-BEZ235 was superior to the allosteric selective mTOR complex inhibitor everolimus in a panel of 21 cancer cell lines of different origin and mutation status. The described Akt activation due to mTOR inhibition was prevented by higher doses of NVP-BEZ235

参考文献

1. Serra, V., Markman, B., Scaltriti, M., Eichhorn, P.J.A., Valero, V., Guzman, M., Botero, M.L., et al. NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations. 2008 Cancer Research 68 (19), pp. 8022-8030

2. ichhorn, P.J.A., Gili, M., Scaltriti, M., Serra, V., Guzman, M., Nijkamp, W., Beijersbergen, R.L., et al. Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235. 2008 Cancer Research 68 (22), pp. 9221-9230