Chemical Name: 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
Biological ActivitySelumetinib is a potent and selective MEK inhibitor (IC50 = 14 nM for MEK1, Kd = 530 nM for MEK2). Inhibits ERK1/2 phosphorylation (IC50 = 10 nM). Exhibits no activity at p38α, MKK6, EGFR, ErbB2 and ERK2. Suppresses several cell lines containing B-Raf and Ras mutations, but displays no effect on a normal fibroblast cell lines. Inhibits tumor growth in colorectal tumor xenograft model. Orally bioavailable.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma.
Huynh H, Soo KC, Chow PK et al.
Mol Cancer Ther
Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor.
Yeh et al.
Clin.Cancer Res., 2007;13:1576
Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines.
Garon et al.
Mol.Cancer Ther., 2010;9:1985
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