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Beschreibung

A cell-permeable quinazoline compound that targets the ATP binding pocket and an adjacent cleft and acts as a potent and reversible inhibitor of Aurora A and Aurora B (IC50 = 110 and 130 nM, respectively) with moderate to excellent selectivity among closely related 16-kinase panel (IC50 = 0.88, 1.03 and 1.79 µ,M for Lck, Src and MEK1, respectively, and IC50 >10 µ,M for Cdk1/2/4, Plk1, Chk1). Blocks phosphorylation of Histone H3-Ser10 in Xenopus cycling egg extracts at 20 µ,M, and reduces mitotic spindle assembly. Shown to repress kinetochore localization of BubR1, Cenp-E, and Mad2, and arrest the growth of proliferating tumor cells.