Refametinib, 1 mg

A research-grade small molecule from STEMCELL Technologies, this compound acts as a selective inhibitor of the MEK/ERK signalling pathway. It targets mitogen-activated protein kinase kinases 1 (MEK1) and 2 (MEK2) with reported IC₅₀ values of 19 and 47 nM, respectively, and binds at an allosteric site adjacent to the ATP pocket. The inhibitor is reported to be selective for MEK1/2 when compared with 205 other kinases.

The substance is supplied as a crystalline solid with a chemical purity of ≥95%. Its molecular formula is C₁₉H₂₀F₃IN₂O₅S, corresponding to a molecular weight of 572.3 g/mol, and the CAS Number is 923032-37-5. The material is also referenced under the synonyms BAY-86-9766 and RDEA119. According to its Safety Data Sheet, the product is not classified as a hazardous substance or mixture under the Globally Harmonized System (GHS).

Published applications in cancer research include inhibition of growth in cancer cell lines in vitro, including lines harbouring the B-RAF V600E mutation, and suppression of tumour growth in xenograft models of human melanoma (A375), human colon cancer (COLO 205), and primary pancreatic cancers. Synergistic effects have been reported when combined with Erlotinib in pancreatic cancer models and with Sorafenib in hepatocellular carcinoma models. STEMCELL Technologies recommends storage at -20°C, protected from prolonged light exposure; the product is stated to be stable as supplied for 12 months from the date of receipt. Solubility guidance from the supplier indicates ≤1.5 mM in DMSO and ≤35 mM in absolute ethanol. The product is intended for research use only.