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Dactolisib
$66 – $343
Products Details
Product Description
– Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
Web ID
– HY-50673
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C30H23N5O
Citations
– 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.|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. |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 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|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.|Sci Adv. 2023 Mar 22;9(12):eadd5028.|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.|J Clin Toxicol 2014, 4:5|J Clin Toxicol. 2014 October 4, 4:5.
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.|[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.|[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.
CAS Number
– 915019-65-7
Molecular Weight
– 469.54
Compound Purity
– 99.94
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
Clinical Information
– Phase 3
Research Area
– Cancer
Solubility
– 5% TFA : 8.33 mg/mL (ultrasonic;warming;heat to 60°C)|DMF : 2 mg/mL (ultrasonic)|DMSO : 7.81 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Autophagy;mTOR;PI3K
Isoform
– mTOR;mTORC1;mTORC2;PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ
Pathway
– Autophagy;PI3K/Akt/mTOR
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
