NCI Drug Dictionary
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MEK inhibitor MEK162
An orally available inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor MEK162, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1 and MEK2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types. Check for active clinical trials or closed clinical trials using this agent.
|Code names:||ARRY-162 |