Dactolisib
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| Names | |
|---|---|
| IUPAC name
2-Methyl-2-{4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile | |
| Other names
NVP-BEZ235; BEZ-235 | |
| Identifiers | |
915019-65-7  | |
| 3D model (Jmol) | Interactive image |
| ChEMBL | ChEMBL1879463 |
| ChemSpider | 10151099  |
| 7950 | |
| PubChem | 11977753 |
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| Properties | |
| C30H23N5O | |
| Molar mass | 469.55 g·mol−1 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| verify (what is ?) | |
| Infobox references | |
Dactolisib (codenamed NVP-BEZ235 and BEZ-235) is an imidazoquinoline derivative acting as a PI3K inhibitor.[1] It also inhibits mTOR.[2] It is being investigated as a possible cancer treatment.[3]
It has been shown to be toxic to Waldenström's macroglobulinemia cells.[4]
It was the first PI3K inhibitor to enter clinical trials, in 2006 (primary outcome results due in 2010).[5]
References
- ↑ Liu, TJ; Koul, D; LaFortune, T; Tiao, N; Shen, RJ; Maira, SM; Garcia-Echevrria, C; Yung, WKA (11 August 2009). "NVP-BEZ235, a Novel Dual Phosphatidylinositol 3-kinase/Mammalian Target of Rapamycin Inhibitor, Elicits Multifaceted Antitumor Activities in Human Gliomas". Molecular Cancer Therapeutics. 8 (8): 2204–10. doi:10.1158/1535-7163.MCT-09-0160. PMC 2752877
. PMID 19671762. - ↑ Awasthi, N; Yen, PL; Schwarz, MA; Schwarz, RE (March 2012). "The Efficacy of a Novel, Dual PI3K/mTOR Inhibitor NVP-BEZ235 to Enhance Chemotherapy and Antiangiogenic Response in Pancreatic Cancer". Journal of Cellular Biochemistry. 113 (3): 784–91. doi:10.1002/jcb.23405. PMID 22020918.
- ↑ Maira, SM; Stauffer, F; Schnell, C; García-Echeverría, C (1 February 2009). "PI3K Inhibitors for Cancer Treatment: Where Do We Stand?" (PDF). Biochemical Society Transactions. 37 (1): 265–72. doi:10.1042/BST0370265. Retrieved 16 July 2016.
- ↑ Sacco, A; Roccaro, A; Ghobrial, IM (November 2010). "Role of Dual PI3/Akt and mTOR Inhibition in Waldenström's Macroglobulinemia". Oncotarget. 1 (7): 578–82. doi:10.18632/oncotarget.101105. PMC 3248138. PMID 21317453.
- ↑ "A Phase I/II Study of BEZ235 in Patients with Advanced Solid Malignancies Enriched by Patients with Advanced Breast Cancer". ClinicalTrials.gov. Retrieved 16 July 2016.
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