BI-847325 is a potent, ATP-competitive MEK/Aurora kinase inhibitor, inhibts human Aurora A (IC50=25 nM) and Aurora C (IC50=16 nM).
BI-847325 also inhibits MEK1 (IC50=25 nM) and MEK2 (IC50=6 nM).
BI-847325 reduces expression of p-ERK and p-Histone 3 in multiple models of vemurafenib resistance.
BI-847325 decreases the expression of MEK and Mcl-1 and increases the expression of BIM.
BI-847325 is orally bioavailable.
