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    Toremifene Citrate (FC 1157a)
    Toremifene Citrate (FC 1157a)

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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 #: V1726
    CAS #: 89778-27-8Purity ≥98%

    Description: Toremifene Citrate (NSC 613680; NK 622; FC 1157a) is an orally bioavailable SERM (selective estrogen receptor modulator) used in the treatment of advanced breast cancer. Toremifene citrate acts by antagonizing the actions of estrogen in the body. Toremifene (7.5 mM) causes approximately 60% of the cells to exhibit morphologic characteristics typical of cells undergoing programmed death, or apoptosis in human breast cancer cells. Toremifene (5-10 mM) results in elevated levels of TRPM-2 and TGF beta 1 mRNAs in in vitro or in vivo grown tumor cells.

    References: J Natl Cancer Inst. 1993 Sep 1;85(17):1412-8; Carcinogenesis. 1995 Nov;16(11):2733-41.

    Related CAS #: 89778-27-8 (citrate)   89778-26-7 (free base) 

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    Molecular Weight (MW)598.08
    FormulaC32H36ClNO8
    CAS No.89778-27-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (167.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: (Z)-2-(4-(4-chloro-1,2-diphenylbut-1-en-1-yl)phenoxy)-N,N-dimethylethan-1-amine 2-hydroxypropane-1,2,3-tricarboxylate

    InChi Key: IWEQQRMGNVVKQW-OQKDUQJOSA-N

    InChi Code: InChI=1S/C26H28ClNO.C6H8O7/c1-28(2)19-20-29-24-15-13-23(14-16-24)26(22-11-7-4-8-12-22)25(17-18-27)21-9-5-3-6-10-21;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-16H,17-20H2,1-2H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/b26-25-;

    SMILES Code: ClCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=CC=C3.O=C(CC(C(O)=O)(O)CC(O)=O)O

    SynonymsNSC-613680; NK-622; NSC-613680; NSC 613680; NSC613680; Fareston; FC 1157a; FC-1157a; FC1157a; NK 622


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    In Vitro

    In vitro activity: Toremifene (7.5 mM) causes approximately 60% of the cells to exhibit morphologic characteristics typical of cells undergoing programmed death, or apoptosis in human breast cancer cells. Toremifene (5-10 mM) results in elevated levels of TRPM-2 and TGF beta 1 mRNAs in in vitro or in vivo grown tumor cells. Toremifene causes growth inhibition of estrogen-sensitive breast cancer cells by inducing some cells to undergo apoptosis and by inhibiting other cells from entering mitosis. Toremifene induces a dose-dependent level of adducts that is lower than that observed for TAM. Toremifene significantly enhances endogenous DNA adduct formation. Toremifene affects the cell turnover by inhibiting mitotic activity and modifying abundant spontaneous apoptosis in DMBA-induced rat mammary carcinoma.

    In VivoToremifene, at the highest tested dose, increases the incidence of hepatocellular carcinomas in the DEN-initiated groups to a level one-third that observed with Tamoxifen administration to DEN-initiated rats. Toremifene increases the incidence of hypernephromas in previously DEN-initiated rats. Toremifene results in aneuploidy in 50% of the cells examined and compared with the 85% level induced by Tamoxifen in female Sprague-Dawley rats.
    Animal modelRats
    Formulation & Dosage
    References

    J Natl Cancer Inst. 1993 Sep 1;85(17):1412-8; Carcinogenesis. 1995 Nov;16(11):2733-41.


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

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