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    Volasertib (BI 6727)
    Volasertib (BI 6727)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1574
    CAS #: 755038-65-4Purity ≥98%

    Description: Volasertib (formerly also known as BI 6727) is a novel and highly potent dihydropteridinone Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. BI 6727 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. BI 6727 is highly potent (enzyme IC50 = 0.87 nmol/L, EC50 = 11-37 nmol/L on a panel of cancer cell lines) and selective dihydropteridinone with distinct properties. 

    References: Clin Cancer Res. 2009 May 1;15(9):3094-102; BMC Cancer. 2012 Mar 5;12:80. doi: 10.1186/1471-2407-12-80.

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    Molecular Weight (MW)618.81
    FormulaC34H50N8O3 
    CAS No.755038-65-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (32.3 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)4% DMSO+Corn oil: 2 mg/mL  
    SynonymsBI6727, BI-6727, BI 6727; N-((1s,4S)-4-(4-(cyclopropylmethyl)piperazin-1-yl)cyclohexyl)-4-(((R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxybenzamide


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    In Vitro

    In vitro activity: Like BI2536, BI6727 is an ATP-competitive kinase inhibitor from the dihydropteridinone class of compounds. In addition to Plk1, BI6727 also potently inhibits two closely related kinases Plk2 and Plk3 with IC50 of 5 nM and 56 nM, respectively. BI6727 at concentrations up to 10 μM displays no inhibitory activity against a panel of >50 other kinases. BI6727 inhibits the proliferation of multiple cell lines derived from various cancer tissues, including HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji cells with EC50 of 23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM, and 37 nM, respectively. BI6727 treatment (100 nM) in NCI-H460 cells induces an accumulation of mitotic cells with monopolar spindles and positive staining for histone H3 phosphoserine 10, confirming that cells are arrested early in the M phase, followed by induction of apoptosis. Low nanomolar concentrations of BI6727 display potent inhibitory activity against neuroblastoma (NB) tumor-initiating cells (NB TIC) with EC50 of 21 nM, whereas only micromolar concentrations of BI6727 are cytotoxic for normal pediatric neural stem cells. BI6727 induces growth arrest of Daoy and ONS-76 medulloblastoma cells similar to BI 2536.


    Kinase Assay: 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 Assay: Cell proliferation assays are done by incubating cells (HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji) 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.

    In VivoAdministration of BI6727 significantly inhibits the growth of multiple human carcinoma xenografts including HCT116, NCI-H460, and taxane-resistant CXB1 colon carcinoma, accompanied by an increase in the mitotic index as well as an increase in apoptosis. In in vivo studies, BI6727 shows better toxicity and pharmacokinetic profile compared to BI2536.
    Animal modelFemale BomTac:NMRI-Foxn1nu mice grafted s.c. with HCT116, NCI-H460, or CXB1 cells
    Formulation & Dosage Formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl, or suspended in 0.5% Natrosol 250 hydroxyethyl-cellulose; 25 mg/kg; i.v. injection or given intragastrally via gavage needle
    References

    Clin Cancer Res. 2009 May 1;15(9):3094-102; BMC Cancer. 2012 Mar 5;12:80. doi: 10.1186/1471-2407-12-80.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Volasertib (BI 6727)


    Volasertib inhibits the growth of cervical cancer cells in vitro.  2015 Nov 15;5(12):3548-59.

     Volasertib (BI 6727)


    Volasertib induces cell cycle arrest at G2/M Phase in cervical cancer cells.   2015 Nov 15;5(12):3548-59.

     Volasertib (BI 6727)


    Volasertib induces apoptosis in cervical cancer cells.  2015 Nov 15;5(12):3548-59.

     Volasertib (BI 6727)


    Volasertib induces ROS accumulation in cervical cancer cells.

    Volasertib (BI 6727)

    Volasertib potentiates the activity of cisplatin to inhibit the growth of cervical cancer cells in vitro.  2015 Nov 15;5(12):3548-59.

     Volasertib (BI 6727)


    Inhibition of ROS partially rescues volasertib-induces apoptosis in cervical cancer cells.  2015 Nov 15;5(12):3548-59.

     Volasertib (BI 6727)


    Volasertib potentiates the activity of cisplatin to inhibit xenograft tumor growth of cervical cancer cells in nude mice.  2015 Nov 15;5(12):3548-59.


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