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  • 5 mg - 80 EUR
  • 25 mg - 320 EUR
  • 100 mg - 660 EUR

Dabrafenib

Dabrafenib is the second selective BRAF inhibitor approved for treatment of BRAF-mutated metastatic melanoma. It is a highly potent ATP-competitive inhibitor of BRAF (V600E) and BRAF(V600K) kinases, with IC50 values of 0.6, and 0.5 nM, respectively. In contrast, B-Raf and c-Raf display 4- and 6-fold weaker sensitivity, respectively. Dabrafenib has been shown to reduce MEK and ERK phosphorylation, induce G1 cell cycle arrest, followed by cell death. In a xenograft model of human melanoma expressing oncogenic BRAF(V600E), it inhibited ERK activation and tumor growth.

catalogue number: D173
synonyms: GSK2118436
CAS: 1195765-45-7
MW: 519.56 g/mol

References
Mol Cancer Ther. 2012 Apr;11(4):909-20. PMID: 22389471
PLoS One. 2013 Jul 3;8(7):e67583. PMID: 23844038
Onco Targets Ther. 2016 May 6;9:2725-33. PMID: 27226731