Volasertib (BI 6727)

Description

Volasertib (755038-65-4) is an extremely potent and selective inhibitor (IC50’s: 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, IC50’s bromodomains 1 and 2 of BRD4 = 300 and 770 nM respectively2).

The Uses of Volasertib (BI 6727)

Volasertib (BI 6727) is a highly potent Polo-like kinase (PLK) inhibitor.

What are the applications of Application

BI6727 is an ATP-competitive Plk1/2/3 inhibitor

References

1) Rudolph?et al.?(2009)?BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity; Clin. Cancer Res.?15?3094 2) Rudolph?et al.?(2015)?Efficacy and Mechanism of Action of Volasertib, a Potent and Selective Inhibitor of Polo-Like Kinases, in Preclinical Models of Acute Myeloid Leukemia; J. Pharmacol. Exp. Ther.?352?579 3) Ciceri?et al.?(2014)?Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol.?10?305