Western blot analysis of extracts from HeLa cells, untreated (-) or treated with TPA #4174 (200 nM, 20 min; +) with or without pretreating the cells with Selumetinib (AZD6244) for 1 hour at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (D13.14.4E) XP® Rabbit mAb #4370 (upper), p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695 (middle), and β-Actin (D6A8) Rabbit mAb #8457 (lower).
Chemical structure of Selumetinib (AZD6244).
Selumetinib (AZD6244) is supplied as a lyophilized powder. For an 18 mM stock, reconstitute 10 mg of powder in 1.21 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Molecular Weight: 457.7 g/mol
Molecular Formula: C17H15BrCIFN4O3
Solubility: Soluble in DMSO at 9 mg/ml.
Selumetinib (AZD6244), also known as ARRY-142886, is a highly potent and selective non-ATP competitive inhibitor of MEK with an IC50 of 14 nM (1). Researchers have shown this small molecule to inhibit growth in cell lines containing B-Raf and Ras mutations with no effect on normal fibroblasts (1). Treatment with Selumetinib (AZD6244) induces apoptosis and differentiation in tumors from cells with B-Raf or K-Ras mutations (2).
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