CCT137690

CCT137690 is a highly selective, orally bioavailable Aurora kinase inhibitor that inhibits Aurora A and B kinases with low nanomolar IC50 values in both biochemical and cellular assays. CCT137690 inhibits histone H3 and transforming acidic coiled-coil 3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells efficiently. CCT137690 displays antiproliferative activity in a range of human tumor cell lines. CCT137690 treatment of MYCN-amplified neuroblastoma cell lines inhibits cell proliferation and decreases MYCN protein expression.