Volasertib

Volasertib is an extremely potent and selective inhibitor of Polo-like kinase, a critical controller of multiple essential steps of mitosis (IC50: Plk1=0.87 nM, Plk2=5 nM, Plk3=56 nM). It has shown efficacy in multiple solid xenograft tumors models1 and in clinical studies in patients with acute myeloid leukemia. Volasertib has also been shown to potently inhibit BRD4 (Kd=79 nM3, IC50’s bromodomains 1 and 2 of BRD4=300 and 770 nM respectively).