BEZ235 (CAS 915019-65-7)
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BEZ235, known as Dactolisib, represents a promising dual PI3K/mTOR inhibitor (IC50 = 4, 5, 7 and 75 nM for PI 3-Kα, -γ, -δ, and -β, respectively) with immense therapeutic potential against various cancer types. Functioning as a small molecule, it has undergone extensive preclinical and clinical trials. BEZ235 exhibits a broad spectrum of biological activities, encompassing anti-tumor, anti-angiogenic, anti-inflammatory, and anti-apoptotic effects. Demonstrating high target specificity, it has displayed remarkable antiproliferative activity in animal models of cancer, targeting tumor cell lines. The mechanism of action of BEZ235 revolves around the inhibition of two signaling pathways: the PI3K/Akt and mTOR pathways. The PI3K/Akt pathway governs cell survival, proliferation, and metastasis, while the mTOR pathway regulates cell growth and metabolism. By inhibiting these pathways, BEZ235 effectively suppresses tumor growth, angiogenesis, and metastasis. Furthermore, BEZ235 has been observed to induce apoptosis and inhibit inflammation in various cell lines. Notably, BEZ235 also acts as an inhibitor of ATR (IC50 = 21nM).
BEZ235 (CAS 915019-65-7) References
- Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. | Maira, SM., et al. 2008. Mol Cancer Ther. 7: 1851-63. PMID: 18606717
- The efficacy of the novel dual PI3-kinase/mTOR inhibitor NVP-BEZ235 compared with rapamycin in renal cell carcinoma. | Cho, DC., et al. 2010. Clin Cancer Res. 16: 3628-38. PMID: 20606035
- Activity of the novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 against T-cell acute lymphoblastic leukemia. | Chiarini, F., et al. 2010. Cancer Res. 70: 8097-107. PMID: 20876803
- Potential mechanism of interleukin-8 production from lung cancer cells: an involvement of EGF-EGFR-PI3K-Akt-Erk pathway. | Zhang, Y., et al. 2012. J Cell Physiol. 227: 35-43. PMID: 21412767
- A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. | Toledo, LI., et al. 2011. Nat Struct Mol Biol. 18: 721-7. PMID: 21552262
- Targeting renal cell carcinoma with NVP-BEZ235, a dual PI3K/mTOR inhibitor, in combination with sorafenib. | Roulin, D., et al. 2011. Mol Cancer. 10: 90. PMID: 21791089
- FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma. | Elliott, NE., et al. 2011. Blood. 118: 3911-21. PMID: 21821710
- The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer. | Roper, J., et al. 2011. PLoS One. 6: e25132. PMID: 21966435
- An animal model of MYC-driven medulloblastoma. | Pei, Y., et al. 2012. Cancer Cell. 21: 155-67. PMID: 22340590
- Genotype-dependent efficacy of a dual PI3K/mTOR inhibitor, NVP-BEZ235, and an mTOR inhibitor, RAD001, in endometrial carcinomas. | Shoji, K., et al. 2012. PLoS One. 7: e37431. PMID: 22662154
- Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors. | Wilson, TR., et al. 2012. Nature. 487: 505-9. PMID: 22763448
- Metrics other than potency reveal systematic variation in responses to cancer drugs. | Fallahi-Sichani, M., et al. 2013. Nat Chem Biol. 9: 708-14. PMID: 24013279
- Functionally defined therapeutic targets in diffuse intrinsic pontine glioma. | Grasso, CS., et al. 2015. Nat Med. 21: 555-9. PMID: 25939062
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
BEZ235, 50 mg | sc-364429 | 50 mg | $207.00 |