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    EPI-001
    EPI-001

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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 #: V1762
    CAS #: 227947-06-0Purity ≥98%

    Description: EPI-001 (EPI001; EPI 001) is a novel, potent small-molecule antagonist of AR-androgen receptor N-terminal domain (NTD) with potential antineoplastic activity. It inhibits AR-NTD with an IC50 of ∼6 μM and also serves as a selective PPAR-gamma modulator. AR is involved in mediating the actions of male sex steroids and over-expression of AR may lead to hormone-refractory prostate cancer.  

    References: Cancer Cell. 2010 Jun 15;17(6):535-46; Oncotarget. 2015 Feb 28;6(6):3811-24.

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    Molecular Weight (MW)394.89
    FormulaC21H27ClO5
    CAS No.227947-06-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 79 mg/mL (200.1 mM)
    Water: <1 mg/mL
    Ethanol: 79 mg/mL (200.1 mM)
    Other infoChemical Name: 3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol
    InChi Key: HDTYUHNZRYZEEB-UHFFFAOYSA-N
    InChi Code: InChI=1S/C21H27ClO5/c1-21(2,15-3-7-19(8-4-15)26-13-17(24)11-22)16-5-9-20(10-6-16)27-14-18(25)12-23/h3-10,17-18,23-25H,11-14H2,1-2H3
    SMILES Code: OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1
    SynonymsEPI-001; EPI 001; EPI001


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    In Vitro

    In vitro activity: EPI-001 blocks transactivation of the AR NTD, interacts with the AF-1 region, inhibits protein-protein interactions with AR, and reduces AR interaction with androgen-response elements on target genes. In LNCaP cells, EPI-001 inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. In LNCaP cells, EPI-001 also acts as a PPAR-gamma modulator to result in inhibition of androgen receptor expression and activity, which inhibits prostate cancer growth.


    Cell Assay: LNCaP cells are treated with bicalutamide (BIC) or EPI-001 for 1 hr before the addition of R1881 (0.1 nM) for 4 days. LNCaP cells are treated with OCM (50%) with, or without, EPI-001 for 3 days (serum-free, androgen-free, phenol red-free conditions).

    In VivoIn male mice bearing CRPC LNCaP s.c. xenografts, EPI-001 (50 mg/kg, i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth by reducing proliferation and increasing apoptosis.
    Animal modelMale mice bearing LNCaP s.c. xenografts
    Formulation & DosageDissolved in DMSO; 50 mg/kg; i.v. injection
    ReferencesCancer Cell. 2010 Jun 15;17(6):535-46; Oncotarget. 2015 Feb 28;6(6):3811-24.


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

    EPI-001

    EPI-001 inhibits transcriptional activity of AR TAU1 and TAU5 domains in reporter-based assays. Oncotarget. 2015 Feb 28;6(6):3811-24.
     

    EPI-001

    Dose-dependent inhibition of AR expression and PCa/CRPC cell growth mediated by EPI-001. Oncotarget. 2015 Feb 28;6(6):3811-24.
     

    EPI-001

    EPI-001 and troglitazone inhibit AR expression and activity in clinical prostate cancer tissues. Oncotarget. 2015 Feb 28;6(6):3811-24.


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