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