Volasertib is an extremely potent and selective inhibitor (IC50s: Plk1= 0.87 nM, Plk2 = 5 nM, Plk3 = 56 nM) of Polo-like kinase 1, a critical controller of multiple essential steps of mitosis.1 It has shown efficacy in multiple solid xenograft tumors models1 and in clinical studies in patients with acute myeloid leukemia2. Volasertib has also been shown to potently inhibit BRD43 (Kd = 79 nM3, IC50s bromodomains 1 and 2 of BRD4 = 300 and 770 nM respectively2).
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