1. Cell Cycle/DNA Damage Apoptosis
  2. Polo-like Kinase (PLK) Apoptosis
  3. Volasertib

Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.

For research use only. We do not sell to patients.

Volasertib Chemical Structure

Volasertib Chemical Structure

CAS No. : 755038-65-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 157 In-stock
Solution
10 mM * 1 mL in DMSO USD 157 In-stock
Solid
5 mg USD 115 In-stock
10 mg USD 202 In-stock
50 mg USD 643 In-stock
100 mg USD 1140 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Volasertib:

Top Publications Citing Use of Products

    Volasertib purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;43(4):1472-1486.  [Abstract]

    The addition of Volasertib (0.5-1.5 µg/mL blunts the increase of the percentage of annexin-V-binding erythrocytes following glucose deprivation, an effect reaching statistical significance at 1 and 1.5 µg/mL Volasertib.

    View All Polo-like Kinase (PLK) Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[1][2].

    IC50 & Target[3]

    PLK1

    0.87 nM (IC50)

    PLK2

    5 nM (IC50)

    PLK3

    56 nM (IC50)

    In Vitro

    Volasertib (BI 6727; 0.01-10000 nM; 72 hours) has EC50 values of 11 to 37 nmol/L in multiple cell lines[1].
    ? Volasertib (10-1000 nM; 24 hours) results accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase[1].
    ? Volasertib (100 nM; 24-72 hours) induces cell apoptosis at 48 hours[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[1]

    Cell Line: Multiple cell lines
    Concentration: 0.01-10000 nM
    Incubation Time: 72 hours
    Result: 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; THP-1, E50=36 nmol/L and Raji, EC50=37 nmol/L) with EC50 values of 11 to 37 nmol/L.

    Apoptosis Analysis[1]

    Cell Line: NCI-H460 cells
    Concentration: 100 nM
    Incubation Time: 24, 48, 72 hours
    Result: G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours.

    Cell Cycle Analysis[1]

    Cell Line: NCI-H460 cells
    Concentration: 10, 30, 100, 300, 1000 nM
    Incubation Time: 24 hours
    Result: Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.
    In Vivo

    Volasertib (BI 6727; A total weekly dose of 50 mg/kg; Oral; once a week, twice a week, or daily; for 40 days) shows comparable efficacy in human colon carcinoma xenograft models[1].
    ? Volasertib (15, 20, or 25 mg/kg/day; i.v.; 2 consecutive days per week; for 40 days) leads to significant tumor growth delay and even tumor regression in human colon carcinoma xenograft models [1].
    ? Volasertib (70 mg/kg given once weekly or 10 mg/kg daily; oral) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model derived from NCI-H460 cells[1].
    ? Volasertib (a single dose of 40 mg/kg; iv) causes a significant (13-fold) increase in mitotic cells in HCT 116 tumor-bearing nude mice[1].
    ? Volasertib has high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female BomTac:NMRI-Foxn1nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)[1]
    Dosage: A total weekly dose of 50 mg/kg
    Administration: Oral; once a week, twice a week, or daily; for 40 days
    Result: Showed comparable efficacy and were well tolerated.
    Animal Model: Female BomTac:NMRI-Foxn1nu mice and male Wistar rats of the strain Crl:WI[1]
    Dosage: 35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis)
    Administration: IV 5-minute infusion; a single dose 5-minute infusion
    Result: Had high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h).
    Clinical Trial
    Molecular Weight

    618.81

    Formula

    C34H50N8O3

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(C1=CC=C(C(OC)=C1)NC2=NC=C(N(C3=O)C)C(N([C@@H]3CC)C(C)C)=N2)N[C@H]4CC[C@@H](CC4)N5CCN(CC5)CC6CC6

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (80.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6160 mL 8.0800 mL 16.1600 mL
    5 mM 0.3232 mL 1.6160 mL 3.2320 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (3.36 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.41%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6160 mL 8.0800 mL 16.1600 mL 40.4001 mL
    5 mM 0.3232 mL 1.6160 mL 3.2320 mL 8.0800 mL
    10 mM 0.1616 mL 0.8080 mL 1.6160 mL 4.0400 mL
    15 mM 0.1077 mL 0.5387 mL 1.0773 mL 2.6933 mL
    20 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0200 mL
    25 mM 0.0646 mL 0.3232 mL 0.6464 mL 1.6160 mL
    30 mM 0.0539 mL 0.2693 mL 0.5387 mL 1.3467 mL
    40 mM 0.0404 mL 0.2020 mL 0.4040 mL 1.0100 mL
    50 mM 0.0323 mL 0.1616 mL 0.3232 mL 0.8080 mL
    60 mM 0.0269 mL 0.1347 mL 0.2693 mL 0.6733 mL
    80 mM 0.0202 mL 0.1010 mL 0.2020 mL 0.5050 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Volasertib
    Cat. No.:
    HY-12137
    Quantity:
    MCE Japan Authorized Agent: