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Organic compounds that consist of sulfuric acid with organic functional group substitutions; includes compounds that are derived from organic sulfuric acids.
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Selumetinib sulfate is a selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. It inhibits ERK1/2 phosphorylation and can penetrate the blood-brain barrier (BBB).
Causes a time- and dose-dependent reduction in DNA synthesis and cell viability
Induces growth arrest and apoptosis associated with the inactivation of ERK in primary cells
Shows anti-proliferative effects through G0/G1 arrest
Results in growth inhibition of cell lines containing B-Raf and Ras mutations
Decreases the growth rate of xenografts in a dose-dependent manner
Suppresses the growth of xenografts
Inhibits ERK1/2 phosphorylation and growth of xenograft tumors in nude mice
Tumor regressions observed in xenograft models
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