42P BAL0891: A novel, small molecule, dual TTK/PLK1 mitotic checkpoint inhibitor (MCI) with potent single agent activity

Abstract

BAL0891 is a dual inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1). These kinases collaborate in activating the mitotic spindle assembly checkpoint (SAC) at the kinetochore (KT) ensuring correct chromosomal segregation. Here the dual activity of BAL0891 on TTK and PLK1 in tumor cells was linked to profound effects on SAC integrity, rapid induction of aberrant mitosis and polyploidy. A potent and potentially broad single agent activity was observed in models of human cancer.