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

Volasertib (Synonyms: BI 6727)

Cat. No.: HY-12137 Purity: 98.76%
Data Sheet SDS Handling Instructions

Volasertib is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM, as well as the two closely related kinases Plk2 and Plk3 with IC50 values 5 and 56 nM, respectively.

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $131 In-stock
5 mg $96 In-stock
10 mg $168 In-stock
50 mg $536 In-stock
100 mg $950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    Volasertib purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Oct 16;43(4):1.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Volasertib is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM, as well as the two closely related kinases Plk2 and Plk3 with IC50 values 5 and 56 nM, respectively.

    IC50 & Target

    IC50: 0.87 nM (PLK1), 5 nM (PLK2), 56 nM (PLK3)

    In Vitro

    The IC50 values of volasertib in HeLa and Caski cells are 0.02 μM and 2.02 μM, respectively. Volasertib induces cell cycle arrest at G2/M Phase in cervical cancer cells. Volasertib augments the fluorescent intensity of DHE in both Caski and HeLa cells in a dose- and time-dependent manner[1]. Volasertib inhibits proliferation in all 40 cell lines tested, with a mean half-maximal growth inhibitory concentration of 313 nM (range: 4-5000 nM). Volasertib is highly active against RMS-1 alveolar rhabdomyosarcoma xenografts, resulting in 100% tumor regression. Volasertib shows synergistic activity with vincristine but antagonistic effects with etoposide[2]. Volasertib inhibits proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC50=23 nM) and lung (NCI-H460, EC50=21 nM), melanoma (BRO, EC50=11 nM), and hematopoietic cancers (GRANTA-519, EC50=15 nM; HL-60, EC50=32 nM; THP-1, EC50=36 nM and Raji, EC50=37 nM) with EC50values of 11 to 37 nM[3]

    In Vivo

    Volasertib (15 mg/kg, i.p.) potentiates the activity of cisplatin to inhibit xenograft tumor growth of cervical cancer cells in nude mice[1]. Volasertib (70 mg/kg, p.o. once a week or 10 mg/kg, p.o. daily) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model. Volasertib (15 mg/kg, i.v.) significantly suppresses tumor growth and is well tolerated[3].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [3]

    Enzyme activity assays for Plk1, Plk2, and Plk3 are done in the presence of serially diluted inhibitor 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 min 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 values. To establish a kinase selectivity profile, additional kinase assays are done by contract research organizations or reagents are purchased from commercial sources and assays are done according to the supplier's instructions. Appropriate positive and negative controls are included in the assay design. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Cell proliferation assays are done by incubating cells in the presence of various concentrations of volasertib for 72 h 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Volasertib is formulated in hydrochloric acid (0.1 N), diluted with 0.9% NaCl for i.v. treatnebt; Volasertib is resuspended in 0.5% Natrosol 250 hydroxyethyl-cellulose for oral treatment.

    Female BomTac: NMRI-Foxn1nu mice are grafted s.c. with 2×106 HCT 116 human colon carcinoma cells (ATCC CCL-247), 1×106 NCI-H460 non-small cell lung cancer cells (ATCC HTB-177), or CXB1 human colon carcinoma tumor pieces derived from patient material by serial transplantation in nude mice. When tumors have reached a volume of appr 50 to 100 mm3, animals are randomized into treatment and control groups of 10 mice each. Volasertib is formulated in hydrochloric acid (0.1 N), diluted with 0.9% NaCl, and injected i.v. into the tail vein at the indicated dose and schedule. For oral treatment, Volasertib is resuspended in 0.5% Natrosol 250 hydroxyethyl-cellulose and given intragastrally via gavage needle. An administration volume of 10 mL per kilogram of body weight is used for both administration routes. Tumor volumes are determined thrice a week using a caliper. The results are converted to tumor volume (mm3) by the formula length×width2×π/6. The weight of the mice is determined as an indicator of tolerability on the same days. Median tumor volumes on the last day of the experiment are used to calculate treated versus control values (= tumor volumetreated mice×100/tumor volumecontrol mice). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    618.81

    Formula

    C₃₄H₅₀N₈O₃

    CAS No.

    755038-65-4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    Volasertib
    Cat. No.:
    HY-12137
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