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

Volasertib (Synonyms: BI 6727)

Cat. No.: HY-12137 Purity: 98.76%
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 of 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 USD 157 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 115 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 202 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 643 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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.

    Volasertib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Apr;17(4):825-837.

    Effect of Plk1 inhibitor on cell proliferation of TAMR-MCF-7 cells. Effects of BI2536 on Plk1 signaling in TAMR-MCF-7 cells. TAMR-MCF-7 cells are incubated with BI2536 (1, 5 and 10 nM) for 24 h and total cell lysates are subjected to immunoblottings for Plk1, Cdc25c and Cyclin B1.

    Volasertib purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2018 May;1862(5):1134-1147.

    The effects of CS1 on polymerized microtubules are also investigated using a cellular tubulin polymer assay. Nocodazole (1 μM) and Paclitaxel (1.5 μM) are used as depolymerization and polymerization controls, respectively.

    Volasertib purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2018 May;1862(5):1134-1147.

    CS1 and Colchicine (Col) induce the phosphorylation of H1 (T18) and H3 (S29) as detected by western blotting.
    • 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 of 5 and 56 nM, respectively.

    IC50 & Target[3]

    PLK1

    0.87 nM (IC50)

    PLK2

    5 nM (IC50)

    PLK3

    56 nM (IC50)

    In Vitro

    Volasertib is potent against HeLa and Caski cells with IC50 values of 0.02 μM and 2.02 μM, respectively. Volasertib (0.03 μM) induces cell cycle arrest at G2/M Phase in cervical cancer cells. Volasertib (0.003-0.03 μM) induces apoptosis in HeLa cells, and Volasertib (0.3-3 μM) results in Caski cell apoptosis. Volasertib (1, 3 μM or 0.01,0.03 μM) augments the fluorescent intensity of DHE in Caski and HeLa cells in a dose-dependent manner[1]. Volasertib shows inhibitory activities against the proliferation of all 40 cell lines tested, with a mean half-maximal growth inhibitory concentration of 313 nM (range: 4-5000 nM)[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 EC50 values of 11 to 37 nM. Volasertib (100 nM) causes G2-M arrest and induces apoptosis in NCI-H460 cells[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. In addition, Volasertib (15 mg/kg, i.v.) markedly suppresses tumor growth and is well tolerated[3].

    Clinical Trial
    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
    [1]

    Volasertib is dissolved in DMSO.

    Cells are firstly seeded into a 96-well plate at a density of 5000 cells per well, and incubated with drugs in three parallel wells for 72 hr. Then MTT is added to each well at a final concentration of 0.5 mg/mL. After incubation for 4 hr, formazan crystals are dissolved in 100 μL of DMSO, and absorbance at 570 nm is measured by plate reader. The concentrations required to inhibit growth by 50% (IC50) are calculated from survival curves[1]. 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. treatment; 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

    SMILES

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

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