AdipoGen Life Sciences

NVP-BEZ235

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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

Product-specific References

Description

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

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)

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