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MEK inhibitor XL518 An orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor XL518 specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
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Code name: | ![](https://webarchive.library.unt.edu/eot2008/20090115045915im_/http://www.cancer.gov/images/spacer.gif) | XL518 | | ![](https://webarchive.library.unt.edu/eot2008/20090115045915im_/http://www.cancer.gov/images/spacer.gif) |
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