A potent, orally available MEK1 inhibitor
Cobimetinib is a potent, orally available inhibitor of MEK1 (IC50 = 4.2 nM).1,2 It shows more than 100-fold selectivity for MEK when tested against a panel of more than 100 serine-threonine and tyrosine kinases. Cobimetinib induces differentiation and apoptosis in cancer cell lines and is more effective when combined with additional inhibitors, like PLX4032 .2,3,4
1.Akinleye, A., Furgan, M., Mukhi, N., et al.MEK and the inhibitors: From bench to bedsideJ. Hematol. Oncol.627(2013) 2.Hoeflich, K.P., Merchang, M., Orr, C., et al.Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibitionCancer Res.72(1)210-219(2012) 3.Medina, T.M., and Lewis, K.D.The evolution of combined molecular targeted therapies to advance the therapeutic efficacy in melanoma: A highlight of vemurafenib and cobimetinibOnco Targets Ther.93739-3752(2016) 4.Sing, A., Ruan, Y., Tippett, T., et al.Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cellsJ. Exp. Clin. Cancer Res.34(1)104(2015)
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