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Nedometinib is a MEK1 inhibitor (IC50 = 135 nM).1 It is selective for MEK1 over a panel of 44 receptors, ion channels, and enzymes at 10 µM, as well as a panel of an additional 150 kinases. Nedometinib (0.1-10 µM) decreases phosphorylation of ERK in malignant peripheral nerve sheath tumor cells. Topical application of nedometinib (0.1-2.3%) reduces the total number of tumors in a mouse model of cutaneous squamous cell carcinoma induced by UV radiation.
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1. Development of a MEK inhibitor, NFX-