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CAS NO.923032-37-5
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RDEA119 potently inhibited MEK activity in enzyme inhibition assays in a non-ATP-competitive manner (MEK1 IC50 = 19 nmol/L, MEK2 IC50 = 47 nmol/L) determined through incorporation of radioactive phosphate from ATP into ERK as substrate. RDEA119 potently inhibited MEK activity as measured by phosphorylation of ERK1/2 across several human cancer cell lines of different tissue origins and BRAF mutational status with EC50 values ranging from 2.5 to 15.8 nmol/L . BAY 86-9766 exhibited potent antiproliferative activity in HCC cell lines with half-maximal inhibitory concentration values ranging from 33 to 762 nM. BAY 86-9766 was strongly synergistic with sorafenib in suppressing tumor cell proliferation and inhibiting phosphorylation of the extracellular signal-regulated kinase (ERK) .