Volasertib (BI 6727) is a potent, selective Polo-like kinase (PLK) inhibitor with IC50 of 0.87, 5 and 56 nM for PLK1, 2 and 3, respectively.
Volasertib (BI 6727) displays no inhibitory activity against a panel of >50 other kinases.
Volasertib (BI 6727) inhibits proliferation of multiple cell lines derived from various cancer tissues, including HCT116 (EC50=23 nM) and NCI-H460 (EC50=21 nM),BRO (EC50=11 nM), and hematopoietic cancer cell HL-60 (EC50=32 nM).
Volasertib (BI 6727) demonstrates marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer.
