AZD6244, 50 mg

A potent, highly selective small molecule inhibitor of the mitogen-activated protein kinases MEK1 (IC ₅₀ = 14 nM) and MEK2 (Kd = 530 nM), supplied by STEMCELL Technologies. The compound acts as a tight-binding noncompetitive inhibitor that does not bind in the ATP binding pocket of MEK, and also shows micromolar binding to epidermal growth factor receptor (EGFR). It is identified chemically as 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide (CAS 606143-52-6), with molecular formula C₁₇H₁₅BrClFN₄O₃ and molecular weight 457.7 g/mol, and is also known by the synonyms ARRY-142886, Cl-1040, G 00039805, NSC 741O78, and Selumetinib.

Published cancer research applications include inhibition of growth of several tumor cell lines but not normal fibroblast lines and inhibition of tumor growth in a colorectal xenograft tumor model, inhibition of proliferation and induction of differentiation and apoptosis in multiple tumor cell lines and tumor xenograft models (especially those containing BRAF or RAS mutations), and inhibition of proliferation of breast cancer and non-small cell lung cancer cell lines (especially those containing RAF and RAS mutations, respectively). The product is supplied as a crystalline solid of ≥ 98% purity, with a reported solubility of ~0.5 mg/mL in 1:1 DMSO:PBS (pH 7.2), ~20 mg/mL in DMSO, and ~16 mg/mL in DMF, and is described as having low solubility in aqueous media. It is stable at -20 °C as supplied, should be protected from prolonged exposure to light, and is stable for 12 months from the date of receipt.

This product is classified as hazardous (Serious Eye Damage/Eye Irritation Category 1; Skin Sensitization Category 1; Toxic to Reproduction Category 2; Target Organ Systemic Toxicity on repeated exposure Category 2), with reported hazard statements including H318 (causes serious eye damage), H317 (may cause an allergic skin reaction), H361 (suspected of damaging fertility or the unborn child), and H373 (may cause damage to the liver, gastrointestinal tract, and other major organs through prolonged or repeated exposure). The reported oral LD50 in rat is > 300 mg/kg. Products are for research use only and not intended for human or animal diagnostic or therapeutic uses unless otherwise stated. Refer to the Safety Data Sheet (SDS) for full handling information.