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Dactolisib (Tosylate)

Product Specifications

UNSPSC Description

Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

Target Antigen

Autophagy; mTOR; PI3K

Type

Reference compound

Related Pathways

Autophagy;PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/BEZ235-Tosylate.html

Solubility

DMSO : 34 mg/mL (ultrasonic;warming)|H2O : < 0.1 mg/mL

Smiles

CN(C1=C2C3=CC(C4=CC5=CC=CC=C5N=C4)=CC=C3N=C1)C(N2C6=CC=C(C=C6)C(C)(C#N)C)=O.CC7=CC=C(S(=O)(O)=O)C=C7

Molecular Weight

641.74

References & Citations

[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.Arch Pharm (Weinheim). 2024 Sep;357(9):e2400066.|J Clin Toxicol 2014, 4:5|J Clin Toxicol. 2014 October 4, 4:5.|Sci Data. 2024 Sep 19.|Actome. 2024.|Adv Sci (Weinh). 2023 Jun 21;e2300881.|Am J Digest Dis. 2015;2(2):95-99.|Am J Transl Res. 2019 Sep 15;11(9):5573-5585.|Anim Cells Syst. 11 Oct 2021.|Biochem Pharmacol. 2022 May 14;201:115093.|Biomed Res Int. 2018 Aug 5;2018:8372085. |Biomed Res Int. 2021 Apr 20.|bioRxiv. 2024 September 10.|Blood. 2019 Oct 17;134(16):1323-1336. |BMC Med. 2021 Oct 15;19(1):247.|Br J Cancer. 2022 Mar 5.|Cancer Cell Int. 2023 Sep 27;23(1):217.|Cancer Gene Ther. 2020 Sep 16. |Cancer Res. 2024 Oct 30.|Cancers (Basel). 2022 Oct 10;14(19):4966.|Cell Commun Signal. 2023 May 24;21(1):120.|Cell Death Dis. 2020 Jun 30;11(6):491.|Cell Res. 2019 Nov;29(11):895-910. |Cell Signal. 2024 Sep 16:111415.|Cell Syst. 2018 Apr 25;6(4):424-443.e7.|Cell Syst. 2020 Jan 22;10(1):66-81.e11.|EBioMedicine. 2015 Nov 19;2(12):1944-56. |Eur J Med Chem. 2023 Jun 5, 115543.|Exp Hematol Oncol. 2016 Jul 29;5:22. |Front Oncol. 06 October 2022.|Front Pharmacol. 2020 Nov 11;11:580407.|Haematologica. 2020 Mar;105(3):674-686.|Harvard Medical School LINCS LIBRARY|Int J Med Sci. 2024 Jul 9;21(10):1814-1823.|J Biol Chem. 2020 May 22;295(21):7431-7441.|J Chemother. 2022 Mar 3;1-9.|J Exp Clin Cancer Res. 2018 Aug 9;37(1):188. |J Mol Cell Cardiol. 2018 May;118:133-146. |J Nanobiotechnology. 2022 Apr 12;20(1):187.|JCI Insight. 2022 Jul 19;e155899.|Leukemia. 2014 Sep;28(9):1819-27. |Mol Cancer Ther. 2020 Jun;19(6):1351-1362.|Molecules. 2019 Apr 1;24(7):1260.|Molecules. 2020 Apr 23;25(8):1980.|Nat Commun. 2017 Jun 8;8:15617.|Nature. 2018 Aug;560(7719):499-503.|Onco Targets Ther. 2020 Apr 30;13:3501-3510. |Oncotarget. 2017 Jul 11;8(28):45470-45483. |Oncotarget. 2018 Feb 1;9(35):23878-23889.|Oncotargets Ther. 2020 Nov 27;13:12225-12241.|Oxid Med Cell Longev. 22 Oct 2021.|Patent. US20210236501A1.|Sci Adv. 2023 Mar 22;9(12):eadd5028.|Sci Rep. 2024 Oct 28;14(1):25815.|Sci Rep. 2019 Oct 22;9(1):15099. |Sci Signal. 2021 Jun 22;14(688):eabe6156.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|University of North Carolina. School of Medicine, Curriculum in Genetics and Molecular Biology 2021 Aug.

Shipping Conditions

Room Temperature

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-15174/Dactolisib-Tosylate-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-15174/Dactolisib-Tosylate-SDS-MedChemExpress.pdf

Clinical Information

Phase 3

CAS Number

1028385-32-1

Available Sizes

Curated Selection

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