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

Volasertib trihydrochloride  (Synonyms: BI 6727 trihydrochloride)

Cat. No.: HY-12137A Purity: 99.12%
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Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.

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

CAS No. : 946161-17-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 35 publication(s) in Google Scholar

Other Forms of Volasertib trihydrochloride:

Volasertib trihydrochloride Related Antibodies

Top Publications Citing Use of Products

35 Publications Citing Use of MCE Volasertib trihydrochloride

WB
Cell Proliferation/Viability Assay
In Vivo Efficacy Study

    Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Nov 21;9(1):373.  [Abstract]

    MCL17-PDX mice were treated as indicated: vehicle (n = 5), abemaciclib (50 mg/kg, oral, daily; n = 5), and volasertib (5 mg/kg, intraperitoneal, weekly; n = 5). Tumor size was measured every 7 days during the treatment. Tumor volume = length x width2/2. Mice were euthanized after 21 days of treatment. Tumors were excised and weighed in comparison between each group.

    Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Signal. 2025 Mar 18;18(878):eadi5174.  [Abstract]

    BI6727 (BI) treatment rescued the protein levels of PDCD4 resulting from nocodazole (Noc)–mediated mitotic arrest. DU145 shCtl and shPLK1 cells were generated with lentivirus expressing control shRNA or one of two specific PLK1 shRNA, followed by nocodazole (100 ng/ml) or 10 nM BI6727 treatment for 16 hours. The protein levels of PLK1 and PDCD4 were determined by immunoblotting, with β-actin and p-H3 as controls for loading and mitotic arrest. Blots are representative of three independent experiments

    Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 16;15(1):2377.  [Abstract]

    Immunoblot of NUDT1 p-S121 in Kelly cells treated with PLK1 shRNA or BI6727 (20 nM, 0, 24, 48 h).

    Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 14;8(1):92.  [Abstract]

    Cell survival curve for HUTU-80 cells treated with the indicated inhibitors with Volasertib from 0 to 100 μM (36 h).

    Volasertib trihydrochloride 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:

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    PLK1 PLK2 PLK3 PLK4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    PLK1

    0.87 nM (IC50)

    PLK2

    5 nM (IC50)

    PLK3

    56 nM (IC50)

    In Vitro

    Volasertib trihydrochloride (BI 6727 trihydrochloride; 0.01-10000 nM; 72 hours) has EC50 values of 11 to 37 nmol/L in multiple cell lines[1].
    Volasertib trihydrochloride (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 trihydrochloride (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.

    Volasertib trihydrochloride Related Antibodies

    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 trihydrochloride (BI 6727 trihydrochloride; 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 trihydrochloride (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 trihydrochloride (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).
    Molecular Weight

    728.20

    Formula

    C34H53Cl3N8O3
    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.[H]Cl.[H]Cl.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 100 mg/mL (137.32 mM)

    DMSO : 100 mg/mL (137.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3732 mL 6.8662 mL 13.7325 mL
    5 mM 0.2746 mL 1.3732 mL 2.7465 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation
    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 (sealed storage, away from moisture). 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
    H2O / DMSO 1 mM 1.3732 mL 6.8662 mL 13.7325 mL 34.3312 mL
    5 mM 0.2746 mL 1.3732 mL 2.7465 mL 6.8662 mL
    10 mM 0.1373 mL 0.6866 mL 1.3732 mL 3.4331 mL
    15 mM 0.0915 mL 0.4577 mL 0.9155 mL 2.2887 mL
    20 mM 0.0687 mL 0.3433 mL 0.6866 mL 1.7166 mL
    25 mM 0.0549 mL 0.2746 mL 0.5493 mL 1.3732 mL
    30 mM 0.0458 mL 0.2289 mL 0.4577 mL 1.1444 mL
    40 mM 0.0343 mL 0.1717 mL 0.3433 mL 0.8583 mL
    50 mM 0.0275 mL 0.1373 mL 0.2746 mL 0.6866 mL
    60 mM 0.0229 mL 0.1144 mL 0.2289 mL 0.5722 mL
    80 mM 0.0172 mL 0.0858 mL 0.1717 mL 0.4291 mL
    100 mM 0.0137 mL 0.0687 mL 0.1373 mL 0.3433 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • 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.

    Keywords:

    Volasertib trihydrochloride946161-17-7BI 6727 trihydrochloridePolo-like Kinase (PLK)ApoptosisorallyATP-competitivemitoticarrestdihydropteridinoneHCT 116NCI-H460BROGRANTA-519HL-60THP-1RajiInhibitorinhibitorinhibit

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