AZD6244, 10 mg

Offered by STEMCELL Technologies, this small molecule is a potent, highly selective inhibitor of the mitogen-activated protein kinases MEK1 and MEK2, with reported values of IC50 = 14 nM for MEK1 and Kd = 530 nM for MEK2. It 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). The material is supplied as a crystalline solid with a stated purity of ≥ 98%.

The chemical name is 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide, and it is also known by the synonyms ARRY-142886, Cl-1040, G 00039805, NSC 741O78, and Selumetinib. Its molecular formula is C17H15BrClFN4O3, molecular weight 457.7 g/mol, and CAS number 606143-52-6. Reported solubilities are approximately 0.5 mg/mL in 1:1 DMSO:PBS (pH 7.2), approximately 20 mg/mL in DMSO, and approximately 16 mg/mL in DMF. The product is stable at -20°C when stored protected from light and remains stable as supplied for 12 months from the date of receipt.

Published cancer research applications include inhibition of growth in several tumor cell lines while sparing normal fibroblasts, suppression of tumor growth in a colorectal xenograft model, and induction of differentiation and apoptosis in tumor models, particularly those harbouring BRAF or RAS mutations. The product is intended for research use only. The accompanying Safety Data Sheet classifies the substance as causing serious eye damage, as a skin sensitizer, as suspected of damaging fertility or the unborn child, and as potentially causing damage to the liver, gastrointestinal tract, and other major organs through prolonged or repeated exposure, with an oral LD50 in rat reported as > 300 mg/kg.