Dabrafenib
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MedKoo CAT#: 205479

CAS#: 1195765-45-7 (free base)

Description: Dabrafenib, also known as GSK2118436 , is an orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity. Dabrafenib selectively binds to and inhibits the activity of B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. B-raf belongs to the the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations. On May 29, 2013, FDA approved this drug.


Price and Availability

Size
Price

50mg
USD 120
500mg
USD 550
5g
USD 2650
50g
USD 9950
Size
Price

100mg
USD 190
1g
USD 950
10g
USD 4650
100g
USD 16850
Size
Price

200mg
USD 350
2g
USD 1650
20g
USD 5950
200g
Ask price

Dabrafenib (free base), purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 10g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205479
Name: Dabrafenib
CAS#: 1195765-45-7 (free base)
Chemical Formula: C23H20F3N5O2S2
Exact Mass: 519.10105
Molecular Weight: 519.56
Elemental Analysis: C, 53.17; H, 3.88; F, 10.97; N, 13.48; O, 6.16; S, 12.34


Related CAS #: 1195765-45-7 (free base)   1195768-06-9 (mesylate)    

Synonym: GSK2118436A ( Dabrafenib ); GSK 2118436A; GSK-2118436A; GSK2118436B ( Dabrafenib Mesylate ); GSK-2118436B; GSK 2118436B. Trade name: Tafinlar.

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

InChi Key: BFSMGDJOXZAERB-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H20F3N5O2S2/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/h4-11,31H,1-3H3,(H2,27,28,29)

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


Technical Data

Appearance:
White to off-white solid powder

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

Safety Data Sheet (MSDS):

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, not in water

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).

Harmonized System Code:
293490


Additional Information

Related CAS#
CAS#1195765-45-7 (Dabrafenib)
CAS#1195768-06-9 (Dabrafenib mesylate)


References

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.