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    MCB-613
    MCB-613

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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 #: V1884
    CAS #: 1162656-22-5Purity ≥98%

    Description: MCB-613 is a novel and potent stimulator of p160 steroid receptor coactivators (SRCs). It is a Pan-SRCs stimulator. MCB-613 is confirmed to be a strong activator of all three SRCs family proteins. MCB-613 can super-activate transcriptional activity of SRCs. MCB-613 markedly increases SRCs’ interactions with other coactivators. Coactivation of MMP2 or MMP13 promoter-driven luciferase reporter with SRC-3 was greatly enhanced by MCB-613. MCB-613 increased SRC-3’s interaction with CBP and CARM1 robustly in a dose-dependent manner. 

    References: Cancer Cell. 2015 Aug 10;28(2):240-52

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    Molecular Weight (MW)304.39 
    FormulaC20H20N2O 
    CAS No.1162656-22-5 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 60 mg/mL (197.1 mM)
    Water: <1 mg/mL
    Ethanol: 60 mg/mL (197.1 mM)
    Solubility (In vivo)4% DMSO+30% PEG 300+ddH2O: 2mg/mL 
    SynonymsMCB-613; MCB 613; MCB613


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    In Vitro

    In vitro activity: MCB-613 selectively and reversibly binds to the RID of SRC-3, and selectively kills cancer cells including MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells, without toxicity to mouse primary hepatocytes and mouse embryonic fibroblasts (MEFs). MCB-613 also increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS).


    Kinase Assay: After various compound treatments, cells are lysed in luciferase lysis buffer and assayed for luciferase activity using the ONE-Glo luciferase assay system. All luciferase activities are normalized to protein concentration determined by Bradford assay.


    Cell Assay: Cells [MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells; mouse primary hepatocytes and mouse embryonic fibroblasts] are seeded in 96-well plates and allowed to reach 60% to 70% confluence. After indicated compound treatments, relative numbers of viable cells are measured by MTS assay using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay.

    In VivoIn an MCF-7 breast cancer mouse xenograft model, MCB-613 (20 mg/kg, i.p.) significantly and dramatically inhibits the growth of the tumor while causing no obvious animal toxicity and body weight less.  
    Animal modelMice bearing MCF-7 xenografts 
    Formulation & DosageDissolved in saline;20 mg/kg; i.p. injection 
    References

    Cancer Cell. 2015 Aug 10;28(2):240-52 


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

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