Dabrafenib

• 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].

• Product Name Alternative:

  GSK2118436A; GSK2118436

• UNSPSC:

  12352005

• Hazard Statement:

  H301, H311, H331

• Target:

  Raf

• Type:

  Reference compound

• Related Pathways:

  MAPK/ERK Pathway

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Dabrafenib.html

• Concentration:

  10mM

• Purity:

  99.97

• Solubility:

  DMSO : ≥ 33 mg/mL

• 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

• Molecular Formula:

  C23H20F3N5O2S2

• Molecular Weight:

  519.56

• Precautions:

  H301, H311, H331

• References & Citations:

  [1]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.|[2]Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.|[3]Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49 (4) :214-9.|[4]Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.|[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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  B-Raf; C-Raf

• Citation 01:

  ACS Comb Sci. 2019 Dec 9;21 (12) :805-816.|Acta Pharmacol Sin. 2021 Jan;42 (1) :108-114.|Adv Sci (Weinh) . 2024 Jun 3:e2400023.|Adv Sci (Weinh) . 2025 Aug 22:e08451.|Biochem Biophys Rep. 2025 Sep 3:44:102235.|Biochem Biophys Res Commun. 2020 Feb 5;522 (2) :395-401. |Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biomed Pharmacother. 2024 Jun 27:177:117033.|Biophys J. 2018 Mar 27;114 (6) :1499-1511. |bioRxiv. 2019 Oct 28.|bioRxiv. 2019 Oct. |bioRxiv. 2019 Sep.|bioRxiv. 2024 August 16.|bioRxiv. 2024 Dec 20:2024.12.19.629301.|bioRxiv. 2025 Aug 25:2025.08.21.671520.|bioRxiv. 2025 May 16.|bioRxiv. 2025 Oct 13.|Cancer Cell. 2021 Aug 9;39 (8) :1135-1149.e8.|Cancer Cell. 2024 Mar 11;42 (3) :358-377.e8.|Cancer Res Commun. 2024 Sep 1;4 (9) :2454-2462.|Cell Biochem Biophys. 2025 Mar;83 (1) :1113-1137.|Cell Death Differ. 2022 Aug;29 (8) :1486-1499.|Cell Metab. 2025 May 6;37 (5) :1171-1188.e9.|Cell Mol Gastroenterol Hepatol. 2022;13 (2) :541-564.|Cell Rep Med. 2023 Feb 21;4 (2) :100911.|Cell Rep Med. 2024 Mar 19;5 (3) :101471.|Cell Rep Med. 2025 Apr 2:102053.|Cell Res. 2025 Jan;35 (1) :23-44.|Cell Syst. 2020 Nov 18;11 (5) :478-494.e9.|Cell. 2024 Jan 4;187 (1) :166-183.e25.|Cell. 2018 Aug 9;174 (4) :843-855.e19.|Cells. 2019 Dec 6;8 (12) :1582.|Elife. 2020 Dec 7;9:e61405.|Endocrine. 2025 Jan;87 (1) :220-233.|Exp Cell Res. 2020 Aug 1;393 (1) :112054.|Harvard Medical School LINCS LIBRARY|Hong Kong Polytechnic University. 2025.|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 Control Release. 2024 Nov:375:643-653.|J Med Chem. 2025 Sep 25;68 (18) :19287-19302.|J Pers Med. 2022 Jan 8;12 (1) :77.|J Transl Med. 2023 Jan 9;21 (1) :9.|Jagiellonian University. 2025.|JCO Precis Oncol. 2024 Apr:8:e2300538.|Mol Cell. 2019 Jan 3;73 (1) :7-21.e7. |Mol Ther Nucleic Acids. 2024 Jul 19;35 (3) :102283.|Mol Ther Oncolytics. 2019 Feb 5;12:235-245.|Nat Biomed Eng. 2018 Aug;2 (8) :578-588.|Nat Commun. 2025 May 8;16 (1) :4288.|Nature. 2025 Nov 26.|Neoplasia. 2025 Oct:68:101223.|Oncol Lett. 2025 Jul 18;30 (4) :450.|Oncotarget. 2017 Apr 4;8 (14) :23436-23447. |Patent. US20240366605A1.|Phytomedicine. 2025 Oct:146:157151.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|Redox Biol. 2021 Oct:46:102110.|Research Square Preprint. 2023 May 5.|Sci Data. 2024 Sep 19;11 (1) :1024.|Sci Signal. 2025 Sep 2;18 (902) :eadw3231.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Science. 2017 Dec 1;358 (6367) :eaan4368.|Toxicol Appl Pharmacol. 2022 Jan 1:434:115797.|Toxicol In Vitro. 2020 Jun;65:104777.|Toxicology. 2024 May:504:153807.|bioRxiv. 2023 Nov 13:2023.11.08.566316.|Cancer Cell. 2020 Mar 16;37 (3) :387-402.e7. |Cancer Res. 2022 Jul 18;82 (14) :2552-2564.|J Am Soc Nephrol. 2024 Jan 1;35 (1) :22-40.|JCI Insight. 2023 Dec 22;8 (24) :e171140.|Patent. US20240307400A1.|Patent. US20240366605A1|University of Washington. 2025.

• CAS Number:

  [1195765-45-7]