ro4987655

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.

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