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    Endoxifen HCl
    Endoxifen HCl

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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 #: V1728
    CAS #: 1032008-74-4Purity ≥98%

    Description: Endoxifen HCl (Z-Endoxifen; N-Desmethyl-4-hydroxytamoxifen), the hydrochloride salt of endoxifen which is an active metabolite of Tamoxifen, is a potent and selective estrogen receptor antagonist/SERM with potential anticancer activity. It has been found to be effective in patients that have failed previous hormonal therapies. Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen.

    References: Cancer Chemother Pharmacol. 2005 May;55(5):471-8; Breast Cancer Res Treat. 2010 Jul;122(2):579-84.

    Related CAS #: 1032008-74-4 (HCl)   1372937-28-4 (citrate)   1032008-66-4 (acetate)   112093-28-4 (free base)   1032008-71-1 (mesylate)  

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    Molecular Weight (MW)409.95
    FormulaC25H28ClNO2
    CAS No.1032008-74-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (180.5 mM)
    Water: <1 mg/mL
    Ethanol: 74 mg/mL (180.5 mM)
    Other info

    Chemical Name: (Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol hydrochloride

    InChi Key: RPFIMPDXTABYCN-BJFQDICYSA-N

    InChi Code: InChI=1S/C25H27NO2.ClH/c1-3-24(19-7-5-4-6-8-19)25(20-9-13-22(27)14-10-20)21-11-15-23(16-12-21)28-18-17-26-2;/h4-16,26-27H,3,17-18H2,1-2H3;1H/b25-24-;

    SMILES Code: OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[H]Cl

    Synonyms

    Z-Endoxifen HCl; 4-Hydroxy-N-desmethyltamoxifen; Endoxifen hydrochloride; N-Desmethyl-4-hydroxytamoxifen


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    In Vitro

    In vitro activity: Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM


    Cell Assay: MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.

    In VivoIn vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen.
    Animal modelMice bearing MCF-7 human mammary tumor xenografts
    Formulation & DosageDissolved in water; 8 mg/kg; Oral gavage 
    References

    Cancer Chemother Pharmacol. 2005 May;55(5):471-8; Breast Cancer Res Treat. 2010 Jul;122(2):579-84.


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

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