| Name | 4-Hydroxytamoxifen |
| Description | 4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research. |
| 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. [1]
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. [2] |
| 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. [3]
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. [4] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 0.1 mg/mL (insoluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.16 mM), Sonication is recommended.
DMSO : 58.3 mg/mL (150.45 mM), Sonication is recommended.
|
| Keywords | progestogenReceptor | progestogen Receptor | nucleus translocation | ICI-79280 | ICI79280 | EstrogenReceptor | Estrogen Receptor/ERR | Estrogen Receptor | ERR | ER | 4-Hydroxytamoxifen | 4Hydroxytamoxifen | 4-hydroxy Tamoxifen | 4 Hydroxytamoxifen | (Z)-Afimoxifene |
| Inhibitors Related | Tamoxifen | Mifepristone | Estradiol | Astragaloside IV | Bisphenol B | Bisphenol Z | Mequinol | Phthalic acid | Ethisterone | Alpha-Estradiol | Ferrous Bisglycinate | Cholesterol |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
