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  • 5 mg - 65 EUR
  • 25 mg - 195 EUR
  • 100 mg - 585 EUR

Binimetinib

Binimetinib is a second generation MEK1/2 inhibitor with demonstrated efficacy against BRAF- and RAS-mutant tumors. Binimetinib is an ATP-uncompetitive inhibitor of MEK1/2, with nanomolar activity against purified MEK enzyme (IC50 = 12 nM), but without any activity on a kinase panel of 220 enzymes at a dose of 10 µM. It inhibits both basal and induced levels of ERK phosphorylation in numerous cancer cell lines with IC50s as low as 5 nM. Binimetinib is especially potent at inhibiting the cell proliferation of mutant B-Raf and Ras cell lines such as HT29, Malme-3M, SK-MEL-2, COLO 205, SK-MEL-28 and A375 (IC50s from 30-250 nM).

catalogue number: B175
synonyms: ARRY162, ARRY438162, MEK162
CAS: 606143-89-9
MW: 441.23 g/mol

References
American Association for Cancer Research Annual Meeting (04/19/2010) www.arraybiopharma.com
Acta Neuropathol Commun. 2014 Apr 8;2:41. PMID: 24713450