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Dabrafenib
$50 – $190
Products Details
Product Description
– Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
Web ID
– HY-14660
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C23H20F3N5O2S2
Citations
– ACS Comb Sci. 2019 Dec 9;21(12):805-816.|Acta Pharmacol Sin. 2021 Jan;42(1):108-114.|Biochem Biophys Res Commun. 2017 Aug 5;489(4):484-489.|Biochem Biophys Res Commun. 2020 Feb 5;522(2):395-401. |Biophys J. 2018 Mar 27;114(6):1499-1511. |bioRxiv. 2019 Oct 28.|bioRxiv. 2019 Oct. |bioRxiv. 2019 Sep.|Cancer Cell. 2021 Aug 9;39(8):1135-1149.e8.|Cell Death Differ. 2022 Jan 22.|Cell Mol Gastroenterol Hepatol. 2021 Oct 23;S2352-345X(21)00223-X.|Cell Rep Med. 2023 Jan 10;100911.|Cell Syst. 2020 Nov 18;11(5):478-494.e9.|Cell. 2018 Aug 9;174(4):843-855.e19.|Cells. 2019 Dec 6;8(12):1582.|Elife. 2020 Dec 7;9:e61405.|Exp Cell Res. 2020 Aug 1;393(1):112054.|Harvard Medical School LINCS LIBRARY|Int J Cancer. 2019 Mar 15;144(6):1379-1390.|Int J Mol Sci. 2022 Nov 19;23(22):14385.|J Cell Mol Med. 2020 Mar;24(6):3336-3345.|J Pers Med. 2022, 12(1), 77.|J Transl Med. 2023 Jan 9;21(1):9.|Mol Cell. 2019 Jan 3;73(1):7-21.e7. |Mol Ther Oncolytics. 2019 Feb 5;12:235-245.|Mol Ther Oncolytics. 2019 Feb 5;12:235-245.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Oncotarget. 2017 Apr 4;8(14):23436-23447. |Redox Biol. October 2021, 102110.|Research Square Preprint. 2023 May 5.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Science. 2017 Dec 1;358(6367):eaan4368.|Toxicol Appl Pharmacol. 2021 Nov 12;115797.|Toxicol In Vitro. 2020 Jun;65:104777.|bioRxiv. 2023 Nov 13.|Cancer Cell. 2020 Mar 16;37(3):387-402.e7. |Cancer Res. 2022 May 18;canres.4152.2021.|J Am Soc Nephrol. 2023 Nov 14.|JCI Insight. 2023 Nov 7:e171140.
References
– [1]Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.|[2]Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9.|[3]Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.|[4]Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920.|[5]Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.
CAS Number
– 1195765-45-7
Molecular Weight
– 519.56
Compound Purity
– 99.97
SMILES
– CC(C)(C)C1=NC(C2=C(F)C(NS(C3=C(F)C=CC=C3F)(=O)=O)=CC=C2)=C(C4=CC=NC(N)=N4)S1
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– DMSO : ≥ 33 mg/mL
Target
– Raf
Isoform
– BRaf;c-Raf
Pathway
– MAPK/ERK Pathway
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.
