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    BI 2536
    BI 2536

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1573
    CAS #: 755038-02-9Purity ≥98%

    Description: BI2536 is a novel and potent small molecule dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively in a cell-free assay. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription and shows 4- and 11-fold greater selectivity against Plk2 and Plk3. BI-2563 is a compound with potential antineoplastic activities. It binds to and inhibits Polo-like kinase 1 (Plk1), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations. Plk1, a serine/threonine-protein kinase, is a key regulator of multiple processes fundamental to mitosis and cell division. 

    References: Curr Biol. 2007 Feb 20;17(4):316-22; Cancer Res. 2009 Mar 1;69(5):1916-23. 

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    Molecular Weight (MW)521.66
    FormulaC28H39N7O3 
    CAS No.755038-02-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 21 mg/mL (40.3 mM)
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (191.7 mM)
    Solubility (In vivo)30% PEG 400+0.5% Tween 80+5% Propylene glycol: 15mg/mL  
    SynonymsBI2536; BI-2536 BI 2536


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    In Vitro

    In vitro activity: BI 2536 blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50 of 3.5 nM and 9.0 nM, respectively. In HeLa cells, BI 2536 treatment ranging from 10-100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, as well as a range of other mitotic processes that are known to depend on Plk1. BI 2536 treatment leads to the HeLa cells arrested in G2/M, subsequently a sub-G1 DNA peak indicative of DNA breakdown and apoptosis, and accumulated cleaved PARP p85 fragments in a concentration-dependent manner. BI 2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM, while blocking the proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells with EC50 of 12-31 nM. Plk1 inhibition by BI 2536 reduces the growth and viability of anaplastic thyroid carcinoma (ATC) cells such as CAL62, OCUT-1, SW1736, 8505C, and ACT-1 with EC50 values of 1.4-5.6 nM.


    Kinase Assay: Recombinant human Plk1 (residues 1-603) is expressed as N-terminal, GST-tagged fusion protein with a baculoviral expression system and purified by affinity chromatography with Glutathione-agarose. Enzyme activity assays for Plk1 are performed in the presence of serially diluted BI 2536 with 20 ng of recombinant kinase and 10 μg casein from bovine milk as the substrate. Kinase reactions are performed in a final volume of 60 μL for 45 minutes at 30 °C (15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-33P-ATP). Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transfer of the precipitates to Multi-Screen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curve is used for calculating IC50 value.


    Cell Assay: Cells (HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells, etc.) are exposed to various concentrations of BI 2536 for 24, and 72 hours. Cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. For determining the DNA content of the cultures, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide (PI) in PBS for 20 minutes at RT. Cell-cycle profiles are determined by flow cytometric analysis.

    In VivoBI 2536 given i.v. once or twice per week is highly efficacious in diverse xenograft models with acceptable tolerability by inhibiting cell proliferation through a mitotic arrest, and subsequently induction of tumor-cell death. Administration of BI 2536 at 50 mg/kg once or twice per week significantly inhibits growth of HCT 116 xenografts with T/C of 15% and 0.3%, respectively. BI 2536 treatment twice-weekly also leads to excellent tumor-growth in BxPC-3 and A549 models with T/C of 5% and 14%, respectively.
    Animal modelFemale BomTac:NMRI-Foxn1nu mice injected subcutaneously with HCT 116, NCI-H460, or A549 cells
    Formulation & DosageFormulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl; 50 mg/kg; i.v. injection
    References

    Curr Biol. 2007 Feb 20;17(4):316-22; Cancer Res. 2009 Mar 1;69(5):1916-23. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    BI 2536

     

    BI 2536

    Crystal structure of BI-2536 bound to BRD4(1) (PDB ID = 4OGI).  2015 May 18;6(7):764-9.

     \BI 2536


    High scoring, GOLD-predicted docking mode of compound 39j in BRD4(1).  2015 May 18;6(7):764-9.


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