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Biological Activity:
An orally active, highly potent and selective inhibitor of MEK 1/2 that has shown tumor-suppressive activity in a wide range of preclinical models. IC50 value to be 14 nM against purified MEK1.
References:
TC Yeh et al. Biological Characterization of ARRY-142886 (AZD6244), a Potent, Highly Selective Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor. Clin. Cancer Res. 2007, 13, 1576-1583. [online]
BR Davies et al. AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models. Mol. Cancer Ther. 2007, 6(8), 2209-2019. [online]
Chemical Name: 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide
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