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Cell Cycle/Checkpoint PLK Volasertib

Volasertib

Catalog No. T6019   CAS 755038-65-4
Synonyms: BI 6727, BI 6727

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, CAS 755038-65-4
Pack Size Availability Price/USD Quantity
2 mg In stock 77.00
5 mg In stock 108.00
10 mg In stock 186.00
25 mg In stock 323.00
50 mg In stock 583.00
100 mg In stock 1031.00
1 mL * 10 mM (in DMSO) In stock 146.00
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Biological Description
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Description 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).
Targets&IC50 PLK1 : ic50 0.87nM,  
In vivo BI 6727 has physicochemical and pharmacokinetic properties that allow in vivo testing of i.v. as well as oral formulations, adding flexibility to dosing schedules. Finally, BI 6727 shows marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer [1]. Volasertib was highly active against RMS-1 alveolar rhabdomyosarcoma xenografts, resulting in 100% tumor regression. Activity was associated with complete and prolonged G2/M arrest and subsequent apoptotic cell death. Volasertib showed synergistic activity with vincristine but antagonistic effects with etoposide [3].
Kinase Assay 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 Research
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
Animal Research
Animal Model: FeBomTac:NMRI-Foxn1nu mice grafted s.c. with HCT116, NCI-H460, or CXB1 cells
Synonyms BI 6727 , BI 6727
Purity 99.72%
Molecular Weight 618.81
Formula C34H50N8O3
CAS No. 755038-65-4

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 16 mg/mL (25.9 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400/0.5% Tween80/5% propylene glycol: 30 mg/mL

Citations

References and Literature
1. Rudolph D, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin Cancer Res. 2009 May 1;15(9):3094-102. 2. Grinshtein N, et al. Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells. Cancer Res. 2011 Feb 15;71(4):1385-95. 3. Abbou S, et al. Polo-like Kinase Inhibitor Volasertib Exhibits Antitumor Activity in Pediatric Malignancies. Anticancer Res. 2016 Feb;36(2):599-609. 4. Xie FF, et al. Volasertib suppresses tumor growth in cervical cancer. Am J Cancer Res. 2015 Nov 15;5(12):3548-59.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Approved drug Library Anti-cancer Clinical Compound Library Cell cycle related Compound Library

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