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  3. Tamoxifen

Tamoxifen (Synonyms: ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen)

Cat. No.: HY-13757A Purity: 99.95%
Handling Instructions

Tamoxifène (ICI 47699) est un modulateur sélectif des récepteurs des œstrogènes (SERM) qui bloque l'action des œstrogènes dans les cellules du sein et peut activer l'activité des œstrogènes dans d'autres cellules, comme les os, le foie, et les cellules utérines. Tamoxifène est un puissant activateur de Hsp90 et améliore l'activité d'ATPase du chaperon moléculaire Hsp90. Tamoxifène active l'autophagie et induit l'apoptosis.

Tamoxifen (ICI 47699) ist ein selektiver estrogen receptor-Modulator (SERM), der die Östrogenwirkung in Brustzellen blockiert und die Östrogenaktivität in anderen Zellen, wie Knochen-, Leber- und Gebärmutterzellen, aktivieren kann. Tamoxifen ist ein potenter Hsp90-Aktivator und steigert die Aktivität des molekularen Hsp90-Chaperons ATPase. Tamoxifen aktiviert die autophagy und induziert die apoptosis.

Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen activates autophagy and induces apoptosis.

For research use only. We do not sell to patients.

Tamoxifen Chemical Structure

Tamoxifen Chemical Structure

CAS No. : 10540-29-1

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Tamoxifen:

Top Publications Citing Use of Products

    Tamoxifen purchased from MCE. Usage Cited in: Cell Commun Signal. 2019 May 23;17(1):50.

    Tamoxifen inhibits the growth and metastasis of prostate tumors in vivo. Western blot analysis of the indicated proteins in prostate primary tumors tissues.

    Tamoxifen purchased from MCE. Usage Cited in: Clinical and Translational Medicine. 2020 Apr.

    Different transmission of MAPK8/FoxO signaling pathway in breast cancer cells (MCF-7, T47D, ZR-75, and MDA-MB-231) and liver cells (LO2) exposed to TAM (Tamoxifen).

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    Description

    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively[5]. Tamoxifen activates autophagy and induces apoptosis[4].

    IC50 & Target[1][4]

    Estrogen receptor

     

    HSP90

     

    In Vitro

    Tamoxifen (ICI 47699) shows strong inhibition of MCF-7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) but does not affect the MDA-MB-231 cells[2].

    In Vivo

    Injection of pre-mutant mice with Tamoxifen (75 mg/kg; injected for 5 days at 6 weeks of age) results in the excision of the floxed exon and, thus, in a gene knockout[3].

    Animal Model: Aldh1l1-cre/ERT2 x Ai95 mice[3]
    Dosage: 75 mg/kg
    Administration: Injected for 5 days at 6 weeks of age
    Result: Resulted in the excision of the floxed exon and a gene knockout.
    Clinical Trial
    Molecular Weight

    371.51

    Formula

    C₂₆H₂₉NO

    CAS No.

    10540-29-1

    SMILES

    CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=CC=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (80.75 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6917 mL 13.4586 mL 26.9172 mL
    5 mM 0.5383 mL 2.6917 mL 5.3834 mL
    10 mM 0.2692 mL 1.3459 mL 2.6917 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (53.83 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.08 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution

    • 5.

      Add each solvent one by one:  50% PEG300    50% saline

      Solubility: 1.67 mg/mL (4.50 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.95%

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    Keywords:

    TamoxifenICI 47699(Z)-Tamoxifentrans-TamoxifenICI47699ICI-47699Estrogen Receptor/ERRHSPAutophagyApoptosisHeat shock proteinsestrogenmodulatorSERMbreastboneliveruterineHsp90chaperoneATPaseInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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