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Volasertib (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) potently inhibited Plk1 as well as the two closely related kinases Plk2 and Plk3 (IC50 values 0.87, 5, and 56 nmol/L, respectively). BI 6727 inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC50 = 23 nmol/L) and lung (NCI-H460, EC50 = 21 nmol/L), melanoma (BRO, EC50 = 11 nmol/L), and hematopoietic cancers (GRANTA-519, EC50 = 15 nmol/L; HL-60, EC50 = 32 nmol/L) with EC50 values of 11 to 37 nmol/L [1]. BI 6727 showed nanomolar activity on NB TICs, with an EC50 of 21 nmol/L, and an excellent selectivity profile, with an EC50 of 2.8 μmol/L on SKPs [2]. Volasertib inhibited proliferation in all 40 cell lines tested, with a mean half-maximal growth inhibitory concentration of 313 nmol/l (range: 4-5000 nmol/l) [3].

In vitro kinase assays: Recombinant human Plk1 (residues 1-603) is expressed as NH2-terminal, GST-tagged fusion protein using a baculoviral expression system and purified by affinity chromatography using glutathione-agarose. Enzyme activity assays for Plk1 are done in the presence of serially diluted BI6727 using 20 ng of recombinant kinase and 10 μg casein from bovine milk as substrate. Kinase reactions are done in a final volume of 60 μL for 45 minutes at 30 °C [15 mM MgCl2, 25 mM MOPS (pH 7.0), 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi γ-32P-ATP]. Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transferring the precipitates to MultiScreen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curves are used for calculating IC50 value.

Cell proliferation assays are done by incubating cells in the presence of various concentrations of BI6727 for 24, 48, and 72 hours and cell growth is assessed by measuring Alamar blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth is inhibited by 50% (EC50) are extrapolated from the dose-response curve fit. To determine the DNA content, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide in PBS for 20 minutes at room temperature. Cell cycle profiles are determined by flow cytometric analysis.(Only for Reference) Cell lines: HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji.icon

BI 6727 , BI 6727

99.72% 

618.81

C34H50N8O3

755038-65-4