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

Volasertib (Synonyms: BI 6727)

Cat. No.: HY-12137 Purity: 99.41%
Handling Instructions

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

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Volasertib:

Top Publications Citing Use of Products

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

    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.

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    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].

    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].

    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.
    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)

    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
    10 mM 0.1616 mL 0.8080 mL 1.6160 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.41%

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