30 CHF CHF 30.00
AG-CR1-3633-M0055 mgCHF 30.00
AG-CR1-3633-M02525 mgCHF 75.00
|Synonyms||Dactolisib; BEZ235; 4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-α,α-dimethyl-benzeneacetonitrile|
|Appearance||White to off-white solid.|
|Solubility||Soluble in dimethylformamide (~10mg/ml). Sligthly soluble in DMSO or chloroform (~1mg/ml). Warming and sonication might be necessary. Insoluble in water.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
Keep cool and dry.
Protect from moisture and oxygen.
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Potent dual ATP-competitive pan class I PI3K and mTOR inhibitor (p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4nM, 5nM, 7nM, 75nM and 6nM, respectively), subsequently inducing G1 phase arrest in biological cell growth and viability assays.
- Anticancer compound. Antiproliferative against several animal tumor cell lines, specifically blocking the dysfunctional activation of the PI3K pathway,
- Enhances the efficacy of other anticancer agents when used in in vivo combination studies.
- Strongly inhibits VEGF-induced cell proliferation and survival in vitro and VEGF-induced angiogenesis in vivo.
- Shown to be a potent inhibitor of ATM- and DNA-PKCs-mediated DNA damage and DNA double-strand break repair.
- Shown to have neuroprotective properties on amyloid-β 1-42 induced neurotoxicity and memory impairment.
- Shows anti-trypanosomal activity for some selected species.
- 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: S.M. Maira, et al.; Mol. Cancer Ther. 7, 1851 (2008)
- Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging: C.R. Schnell, et al.; Cancer Res. 68, 6598 (2008)
- NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations: V. Serra, et al.; Cancer Res 68, 8022 (2008)
- Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway: S.M. Maria, et al.; Future Med. Chem. 1, 137 (2009)
- Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: R. Marone, et al.; Mol. Cancer Res. 7, 601 (2009)
- Chiarini F, Grimaldi C, Ricci F, et al. Activity of the novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 against T-cell acute lymphoblastic leukemia: F. Chiarini, et al.; Cancer Res. 70, 8097 (2010)
- NVP-BEZ235, a dual pan class I PI3 kinase and mTOR inhibitor, promotes osteogenic differentiation in human mesenchymal stromal cells: S.K. Martin, et al.; J. Bone Miner. Res. 25, 2126 (2010)
- Recent results in protein kinase inhibition for tropical diseases: D.P. Rotella, et al.; Bioorg. Med. Chem. Lett. 22, 6788 (2012)
- The dual PI3K/mTOR inhibitor NVP-BEZ235 is a potent inhibitor of ATM- and DNA-PKCs-mediated DNA damage responses: B. Mukherjee, et al.; Neoplasia 14, 34 (2012)
- Inhibition of autophagy as a strategy to augment radiosensitization by the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235: G.J. Cerniglia, et al.; Mol. Pharmacol. 82, 1230 (2012)
- Inhibition of DNA double-strand break repair by the dual PI3K/mTOR inhibitor NVP-BEZ235 as a strategy for radiosensitization of glioblastoma: C.R. Gil del Alcazar, et al.; Clin. Cancer Res. 20, 1235 (2014)
- Neuroprotective effects of the anticancer drug NVP-BEZ235 (dactolisib) on amyloid-β 1-42 induced neurotoxicity and memory impairment: P.M. Bellozi, et al.; Sci. Rep. 6, 25226 (2016)