Dabrafenib mesylate

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 100945

CAS#: 1195768-06-9 (mesylate)

Description: Dabrafenib mesylate, also known as GSK 2118436B, is a potent and orally active B-raf (BRAF) inhibitor with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases such as SIK1, NEK11, and LIMK1 at higher concentrations. Some mutations in the BRAF gene, including those that result in BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Dabrafenib inhibits BRAF V600 mutation-positive melanoma cell growth in vitro and in vivo.

Chemical Structure

Dabrafenib mesylate
CAS# 1195768-06-9 (mesylate)

Theoretical Analysis

MedKoo Cat#: 100945
Name: Dabrafenib mesylate
CAS#: 1195768-06-9 (mesylate)
Chemical Formula: C24H24F3N5O5S3
Exact Mass:
Molecular Weight: 615.6612
Elemental Analysis: C, 46.82; H, 3.93; F, 9.26; N, 11.38; O, 12.99; S, 15.62

Price and Availability

Size Price Availability Quantity
200.0mg USD 150.0 Same day
500.0mg USD 250.0 Same day
1.0g USD 450.0 Same day
2.0g USD 750.0 Same day
5.0g USD 1450.0 Same day
10.0g USD 2650.0 Same day
20.0g USD 4650.0 Same day
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Related CAS #: 1195765-45-7 (free base)   1195768-06-9 (mesylate)    

Synonym: Dabrafenib mesylate; GSK 2118436B; GSK2118436B; GSK-2118436B; GSK2118436 Methane sulfonate salt; Brand name: Taflinar.

IUPAC/Chemical Name: N-(3-(5-(2-aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide methanesulfonate


InChi Code: InChI=1S/C23H20F3N5O2S2.CH4O3S/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25;1-5(2,3)4/h4-11,31H,1-3H3,(H2,27,28,29);1H3,(H,2,3,4)

SMILES Code: O=S(C1=C(F)C=CC=C1F)(NC2=CC=CC(C3=C(C4=NC(N)=NC=C4)SC(C(C)(C)C)=N3)=C2F)=O.CS(=O)(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 615.6612 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Banzi M, De Blasio S, Lallas A, Longo C, Moscarella E, Alfano R, Argenziano G. Dabrafenib: a new opportunity for the treatment of BRAF V600-positive melanoma. Onco Targets Ther. 2016 May 6;9:2725-33. doi: 10.2147/OTT.S75104. eCollection 2016. Review. PubMed PMID: 27226731; PubMed Central PMCID: PMC4866744.

2: Spain L, Julve M, Larkin J. Combination dabrafenib and trametinib in the management of advanced melanoma with BRAFV600 mutations. Expert Opin Pharmacother. 2016;17(7):1031-8. doi: 10.1517/14656566.2016.1168805. Epub 2016 Apr 12. Review. PubMed PMID: 27027150.

3: Zia Y, Chen L, Daud A. Future of combination therapy with dabrafenib and trametinib in metastatic melanoma. Expert Opin Pharmacother. 2015;16(14):2257-63. doi: 10.1517/14656566.2015.1085509. Epub 2015 Sep 2. Review. PubMed PMID: 26331795.

4: Giurcaneanu C, Nitipir C, Popa LG, Forsea AM, Popescu I, Bumbacea RS. Evolution of melanocytic nevi under vemurafenib, followed by combination therapy with dabrafenib and trametinib for metastatic melanoma. Acta Dermatovenerol Croat. 2015;23(2):114-21. Review. PubMed PMID: 26228819.

5: Khoja L, Hogg D. Dabrafenib in the treatment of metastatic or unresectable melanoma. Expert Rev Anticancer Ther. 2015 Mar;15(3):265-76. doi: 10.1586/14737140.2015.1014343. Review. PubMed PMID: 25711514.

6: Awad MM, Sullivan RJ. Dabrafenib in combination with trametinib for the treatment of metastatic melanoma. Expert Rev Clin Pharmacol. 2015 Jan;8(1):25-33. doi: 10.1586/17512433.2015.974556. Epub 2014 Dec 4. Review. PubMed PMID: 25473943.

7: McGettigan S. Dabrafenib: A New Therapy for Use in BRAF-Mutated Metastatic Melanoma. J Adv Pract Oncol. 2014 May;5(3):211-5. Review. PubMed PMID: 25089220; PubMed Central PMCID: PMC4114496.

8: Luke JJ, Ott PA. New developments in the treatment of metastatic melanoma - role of dabrafenib-trametinib combination therapy. Drug Healthc Patient Saf. 2014 Jun 24;6:77-88. doi: 10.2147/DHPS.S39568. eCollection 2014. Review. PubMed PMID: 25018652; PubMed Central PMCID: PMC4075957.

9: Rutkowski P, Blank C. Dabrafenib for the treatment of BRAF V600-positive melanoma: a safety evaluation. Expert Opin Drug Saf. 2014 Sep;13(9):1249-58. doi: 10.1517/14740338.2014.939954. Epub 2014 Jul 11. Review. PubMed PMID: 25014231.

10: Kainthla R, Kim KB, Falchook GS. Dabrafenib. Recent Results Cancer Res. 2014;201:227-40. doi: 10.1007/978-3-642-54490-3_14. Review. PubMed PMID: 24756796.

11: Kainthla R, Kim KB, Falchook GS. Dabrafenib for treatment of BRAF-mutant melanoma. Pharmgenomics Pers Med. 2013 Dec 31;7:21-9. doi: 10.2147/PGPM.S37220. eCollection 2014. Review. PubMed PMID: 24516336; PubMed Central PMCID: PMC3917541.

12: Trinh VA, Davis JE, Anderson JE, Kim KB. Dabrafenib therapy for advanced melanoma. Ann Pharmacother. 2014 Apr;48(4):519-29. doi: 10.1177/1060028013513009. Epub 2013 Nov 20. Review. PubMed PMID: 24259661.

13: Medina T, Amaria MN, Jimeno A. Dabrafenib in the treatment of advanced melanoma. Drugs Today (Barc). 2013 Jun;49(6):377-85. doi: 10.1358/dot.2013.49.6.1968669. Review. PubMed PMID: 23807941.

14: Luke JJ, Hodi FS. Ipilimumab, vemurafenib, dabrafenib, and trametinib: synergistic competitors in the clinical management of BRAF mutant malignant melanoma. Oncologist. 2013 Jun;18(6):717-25. doi: 10.1634/theoncologist.2012-0391. Epub 2013 May 24. Review. PubMed PMID: 23709751; PubMed Central PMCID: PMC4063399.

15: Gibney GT, Zager JS. Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies. Expert Opin Drug Metab Toxicol. 2013 Jul;9(7):893-9. doi: 10.1517/17425255.2013.794220. Epub 2013 Apr 29. Review. PubMed PMID: 23621583.

16: Menzies AM, Long GV, Murali R. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012;6:391-405. doi: 10.2147/DDDT.S38998. Epub 2012 Dec 11. Review. PubMed PMID: 23251089; PubMed Central PMCID: PMC3523565.

17: Heneberg P. [Dabrafenib: the new inhibitor of hyperactive B-RAF kinase]. Klin Onkol. 2012;25(5):333-9. Review. Czech. PubMed PMID: 23102194.

Additional Information

Dabrafenib mesylate is a white to slightly colored solid with three pKas: 6.6, 2.2, and -1.5. It is very slightly soluble at pH 1 and practically insoluble above pH 4 in aqueous media.