1. Cell Cycle/DNA Damage
    Epigenetics
  2. Polo-like Kinase (PLK)
    Epigenetic Reader Domain

BI 2536 

Cat. No.: HY-50698 Purity: 99.19%
Data Sheet SDS Handling Instructions

BI 2536 is a potent and selective inhibitor of Plk1 with IC50 of 0.83 nM, and is also a potent inhibitor of BRD4 with IC50 of 25 nM.

For research use only. We do not sell to patients.
BI 2536 Chemical Structure

BI 2536 Chemical Structure

CAS No. : 755038-02-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO $126 In-stock
5 mg $110 In-stock
10 mg $198 In-stock
50 mg $528 In-stock
100 mg $856 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

    BI 2536 purchased from MCE. Usage Cited in: bioRxiv. Oct. 13, 2017.

    Cells are transfected and treated with BI 2536 as indicated and were fractionated into cytoplasmic (C) and nuclear (N) fractions analyzed by Western blots. The position of Cdc25 and its phosphorylated forms are indicated by arrows. MEK and Histone H3 are respectively cytoplasmic and nuclear proteins probed as controls.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BI 2536 is a potent and selective inhibitor of Plk1 with IC50 of 0.83 nM, and is also a potent inhibitor of BRD4 with IC50 of 25 nM.

    IC50 & Target

    IC50: 0.83 nM (Plk1), 3.5 nM (Plk2/Snk), 9 nM (Plk3/Fnk)[1]
    IC50: 25 nM (BRD4)[2]

    In Vitro

    Exceeding a 100-fold concentration range starting at 10 nM, BI 2536 causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status). The half-maximal effective concentration (EC50) values in this cell panel ranged 2-25 nM, whereas a concentration of 100 nM of BI 2536 is typically sufficient for inducing a complete mitotic arrest. The proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells is blocked at EC50values ranging 12-31 nM, indicating a comparable sensitivity of cycling nontransformed cells to BI 2536[3].

    In Vivo

    BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment; both schedules are well-tolerated, as judged by clinical signs and absence of major body-weight changes[3].

    Clinical Trial
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.9170 mL 9.5850 mL 19.1699 mL
    5 mM 0.3834 mL 1.9170 mL 3.8340 mL
    10 mM 0.1917 mL 0.9585 mL 1.9170 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [3]

    Enzyme activity assays for Plk1, Plk2, and Plk3 are performed in the presence of serially diluted inhibitor (BI 2536) with 20 ng of Recombinant kinase and 10 mg casein from bovine milk as the substrate. Kinase reactions are performed in a final volume of 60 mL for 45 min at 30°C (15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 mCi γ-P33-ATP). Reactions are terminated by the addition of 125 mL of ice-cold 5% TCA. After transfer of the precipitates to Multi-Screen mixed ester cellulose filter plates, plates are washed with1%TCA and quantified radiometrically. Dose-response curves are used for calculating IC50 values[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    BI 2536 is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.1%) before use[3].

    Cell proliferation assays are performed by incubation in the presence of various concentrations of BI 2536 (10 nM-1 μM) for 72 hr, and cell growth is assessed by the measurement of 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[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    BI 2536 is formulated in hydrochloric acid (0.1 N), diluted with 0.9% NaCl (Mice)[3].

    Mice[3]
    Female BomTac:NMRI-Foxn1nu mice are grafted subcutaneously with HCT 116 colon-carcinoma, NCI-H460, or A549 lung-carcinoma cells by subcutaneous injection, respectively, of 2×106, 1×106, and 1×107 cells into the flank of each mouse. When tumors reached a volume of approximately 50 mm3, animals are pair-matched into treatment and control groups of ten mice each. In regression experiments, treatment is not initiated until the mean tumor volume reached 500 mm3. BI 2536 is injected intravenously into the tail vein at the indicated dose and schedule. The administration volume is 10 mL per kg body weight. Tumor volumes are determined three times a week with a caliper. The results are converted to tumor volume (mm3) by the following formula: length×width2×π/6. The weight of the mice is determined as an indicator of tolerability on the same days. For statistical analysis, the treatment group is compared with the vehicle control group in a one-sided (decreasing) exact Wilcoxon test. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    521.65

    Formula

    C₂₈H₃₉N₇O₃

    CAS No.

    755038-02-9

    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.

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number

     

    Organization name *

    Country *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    BI 2536
    Cat. No.:
    HY-50698
    Quantity: