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Description: Dabrafenib mesylate (formerly known as GSK2118436 mesylate) is a novel, specific, orally bioavailable inhibitor of BRAF V600 mutants with IC50 of 0.8 nM in cell-free assays and is 4- and 6-fold less potent against B-Raf (wildype) and c-Raf, respectively. It potently inhibits BRAFV600E, BRAFV600K and BRAFV600D with IC50 values of 0.5nM, 0.6nM and 1.9nM, respectively. Dabrafenib is currently approved by FDA and is widely used in cancer patients harboring BRAF mutations. It is reported that treatment of dabrafenib shrinks the overall size of brain metastases in patients. FDA approved Dabrafenib in 2013 to treat melanoma.
References: Arch Pharm Res. 2011 May; 34(5):699-701.
Related CAS#:1195765-45-7 (free base)
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