4-Hydroxytamoxifen

SKU: orb1302874

Description

4-Hydroxytamoxifen is the primary active metabolite of the SERM Tamoxifen. It acts as a potent estrogen receptor antagonist with oral bioavailability and is widely used in breast cancer research, demonstrating antitumor efficacy in both in vitro cell culture and in vivo animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 68047-06-3
• MW: 387.51
• Purity: 99.93%
• Formula: C₂₆H₂₉NO₂
• SMILES: C(=C(/CC)\C1=CC=CC=C1)(\C2=CC=C(OCCN(C)C)C=C2)/C3=CC=C(O)C=C3
• Target: Estrogen/progestogen Receptor,Estrogen Receptor/ERR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.16 mM);H2O:< 0.1 mg/mL (insoluble);DMSO:58.3 mg/mL (150.45 mM)

Bioactivity

• Target IC50:
  HEK293 cells:0.07 μM|Vero cells:15.1 μM|MDA-MB-231 cells:18.43 μM|Ishikawa cells:3.57 μg/mL|Ishikawa cells:11.5 μM (EC50)|MCF-10A cells:10 μM|ERR:3.3 nM|T47D cells:0.01 μM|DU-145 cells:10 μM (EC50)|DU-145 cells:15.3 μM|MCF-7 cells:0.0034 μM
• In Vivo:
  METHODS: To detect the antitumor activity in vivo, 4-Hydroxytamoxifen (1 mg/kg) was injected intraperitoneally into Nu/Nu mice carrying human breast cancer tumor MCF-7 once a day for twenty-three days. RESULTS: 4-Hydroxytamoxifen effectively inhibited tumor growth in mice. METHODS: To induce Cre recombinase activity, 4-Hydroxytamoxifen (30-60 mg/kg) was injected intraperitoneally into Rosa26BEST1-CreERT2 mice once daily for four days. RESULTS: TdTomato was strongly expressed in the RPE of mice of both sexes.
• In Vitro:
  METHODS: The human endometrial adenocarcinoma cell line HEC-1B was treated with 4-Hydroxytamoxifen (0.01-100 µM) for 3 days, and cell viability was measured using the CellTiter 96 AQueous One Solution Cell Proliferation Assay. RESULTS: HEC-1B cells exposed to higher concentrations (1-100 µM) of 4-Hydroxytamoxifen showed significant differences in cell viability between concentrations. METHODS: ER-positive breast cancer cell lines MCF-7, T47D and BT-474 were treated with 4-Hydroxytamoxifen (0.5-1 µM) and sulforaphane (5 µM) for 48 h. The expression levels of target proteins were detected using Western Blot. RESULTS: Sulforaphane induced PARP cleavage, the intensity of which was dependent on the cell line, and the combination of sulforaphane and 4-Hydroxytamoxifen further enhanced PARP cleavage.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

progestogen Receptor, progestogenReceptor, trans-4-Hydroxytamoxifen, nucleus translocation, ICI 79280, ICI79280, ICI-79280, estrogen receptor, Estrogen Receptor, Estrogen Receptor/ERR, EstrogenReceptor, ER, ERR, 4-hydroxy Tamoxifen, 4Hydroxytamoxifen, 4-Hydroxytamoxifen, 4 Hydroxytamoxifen, (Z)-Afimoxifene, (Z)-4-hydroxy Tamoxifen

Compound Identifiers

PubChem CID

449459