Refametinib, 10 mg

STEMCELL Technologies supplies Refametinib as a small molecule inhibitor of the MEK/ERK signalling pathway. The compound acts as an allosteric inhibitor of both mitogen-activated protein kinase kinase 1 (MEK1) and mitogen-activated protein kinase kinase 2 (MEK2), with reported IC₅₀ values of 19 nM and 47 nM, respectively, and is selective for MEK1/2 versus 205 other kinases. It binds in an allosteric site adjacent to the ATP pocket.

The chemical name is N-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]-cyclopropanesulfonamide, with CAS number 923032-37-5, molecular formula C₁₉H₂₀F₃IN₂O₅S, and molecular weight 572.3 g/mol. The product is supplied as a crystalline solid at a purity of ≥ 95%. Recommended storage is at -20°C, protected from prolonged exposure to light, and it is stable as supplied for 12 months from the date of receipt. Reported solubility limits are ≤ 1.5 mM in DMSO and ≤ 35 mM in absolute ethanol; the compound has low solubility in aqueous media.

Published cancer research applications include inhibition of in vitro growth of cancer cell lines, including those harbouring the B-RAF V600E mutation, and inhibition of tumour growth in xenograft models such as human melanoma A375, human colon cancer COLO 205, and primary pancreatic cancers. The compound synergistically induces apoptosis in pancreatic cancer cell lines when combined with the EGFR inhibitor Erlotinib, and synergistically inhibits tumour growth in hepatocellular carcinoma rodent models when combined with the VEGFR/PDGFR inhibitor Sorafenib. Alternative names for the compound include BAY-86-9766 and RDEA119.