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Description: RO4987655 (also known as CH-4987655) is a novel, orally bioavailable and specific small molecule inhibitor of MEK kinase with an IC50 of 5.2 nM for MEK1/MEK2. It targets the mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1) with potential antineoplastic activity. It potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth with an in vitro IC50 of 5.2 nmol/L for inhibition of MEK1/2. Single-agent oral administration of CH4987655 resulted in complete tumor regressions in xenograft models. In clinical trials, doses of 0.5, 1, 2, 3, and 4 mg were safe and well tolerated. No clinically significant safety event was observed.
References: Clin Cancer Res. 2009 Dec 1; 15(23):7368-74.Clin Cancer Res. 2012 Sep 1; 18(17):4794-805; J Nucl Med. 2012 Dec; 53(12):1836-46.
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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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