NVP-BEZ235

CHF 30.00
In stock
AG-CR1-3633-M0055 mgCHF 30.00
AG-CR1-3633-M02525 mgCHF 75.00
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Product Details
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
Product Type Chemical
Properties
Formula

C30H23N5O

MW 469.5
CAS 915019-65-7
Purity Chemicals ≥98%
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.
InChi Key JOGKUKXHTYWRGZ-UHFFFAOYSA-N
Smiles CN(C1=CN=C(C=CC(C2=CC(C=CC=C3)=C3N=C2)=C4)C4=C1N5C6=CC=C(C(C)(C)C#N)C=C6)C5=O
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Protect from moisture and oxygen.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • 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.
Product References
  1. 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)
  2. 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)
  3. 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)
  4. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway: S.M. Maria, et al.; Future Med. Chem. 1, 137 (2009)
  5. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: R. Marone, et al.; Mol. Cancer Res. 7, 601 (2009)
  6. 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)
  7. 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)
  8. Recent results in protein kinase inhibition for tropical diseases: D.P. Rotella, et al.; Bioorg. Med. Chem. Lett. 22, 6788 (2012)
  9. 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)
  10. 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)
  11. 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)
  12. 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)
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