Definition

An orally bioavailable small molecule inhibitor of the serine/threonine protein kinase Aurora A, with potential antimitotic and antineoplastic activities. Upon oral administration, Aurora A kinase inhibitor JAB-2485 binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, inhibition of cell division and the induction of apoptosis in cells overexpressing Aurora A kinase. Aurora A kinase localizes to the spindle poles and to spindle microtubules during mitosis; it plays an essential role in the regulation of spindle assembly. Aurora kinase A is overexpressed in a wide variety of cancers.