Dactolisib hydrochloride (Synonyms: BEZ235 hydrochloride; NVP-BEZ235 hydrochloride)

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Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC₅₀ of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2.

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Dactolisib hydrochloride Chemical Structure

CAS No. : 2319647-83-9

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Other In-stock Forms of Dactolisib hydrochloride:

Dactolisib

Other Forms of Dactolisib hydrochloride:

Dactolisib In-stock

55 Publications Citing Use of MCE Dactolisib hydrochloride

: Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 9;37(1):188. [Abstract]; Representative images of the western blotting analysis of TSSC3, ATG5, P62, LC3, Src, Akt, mTOR and their phosphorylated versions in MTF and SaOS2 cells. Cells are treated with TSSC3-overexpression, IGF-1, p-YEEI, and BEZ235 separately or in combination.

: Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2018 Aug 5;2018:8372085. [Abstract]; Changes of p-AKT and p-p70 S6K proteins after treatment with NVP-BEZ235 in Ishikawa and Ishikawa-TAX cells. Changes of p-AKT and p-p70 S6K proteins after treatment of Ishikawa and Ishikawa-TAX cells with NVP-BEZ235.

: Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]; Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

: Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 11;8(28):45470-45483. [Abstract]; Activity of PI3K/AKT/mTOR is monitored by examining phosphorylation of AKT-S473, AKT-T308, and S6 by western blotting.

: Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Leukemia. 2014 Sep;28(9):1819-27. [Abstract]; Western blot analysis of human T-ALL cell lines treated for 24 hours using DMSO (vehicle control), 1 μM JQ1, 500 nM BEZ235, or both drugs in combination, using the indicated antibodies. Western blot analysis of these T-ALL cell lines following treatment with JQ1, BEZ235 or both drugs in combination reveals cooperative upregulation of BIM protein expression coupled to induction of apoptosis, as assessed by PARP cleavage.

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mTOR mTORC1 mTORC2

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Description	Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC₅₀ of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2^[1].
Molecular Weight	506.00
Formula	C₃₀H₂₄ClN₅O
CAS No.	2319647-83-9
SMILES	CN(C1=O)C2=C(C3=CC(C4=CC5=C(N=C4)C=CC=C5)=CC=C3N=C2)N1C6=CC=C(C=C6)C(C)(C#N)C.Cl
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (276 KB) Handling Instructions (2659 KB)
References	[1]. Maira SM, et al. 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. Mol Cancer Ther, 2008, 7(7), 1851-1863. [Content Brief] [2]. Roper J, et al. The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer. PLoS One, 2011, 6(9), e25132. [Content Brief] [3]. Lee M, et al. Targeting PI3K/mTOR Signaling Displays Potent Antitumor Efficacy against Nonfunctioning Pituitary Adenomas. Clin Cancer Res. 2015 Jul 15;21(14):3204-15. [Content Brief]

Dactolisib hydrochloride Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dactolisib2319647-83-9BEZ235NVP-BEZ235BEZ 235BEZ-235PI3KmTORAutophagyPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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