volasertib

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2 PLK3 (IC50s: 5 56 nM).

Volasertib (BI 6727) trihydrochloride is a dihydropteridinone derivative that potently and selectively inhibits Polo-like kinase 1 (PLK1), PLK2, and PLK3, acting as an orally active ATP-competitive inhibitor with an IC50 of 0.87 nM against PLK1, 5 nM against PLK2, and 56 nM against PLK3. Its mechanism includes inducing mitotic arrest and apoptosis, with significant antitumor activity observed in various cancer models.

CD 10899, a hydroxylated metabolite of Volasertib, is pharmacologically active against Polo-like kinase 1 (PLK1) with an IC50 of 6 nM. Volasertib is an orally active, highly potent, and ATP-competitive PLK1 inhibitor. CD 10899 can be used for cancer research [1].