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4-Hydroxytamoxifen

4-Hydroxytamoxifen
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.
Catalog No. T4420Cas No. 68047-06-3
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Purity:99.84%
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4-Hydroxytamoxifen

Catalog No. T4420Cas No. 68047-06-3
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$64In Stock
10 mg$89In Stock
25 mg$197In Stock
50 mg$386In Stock
100 mg$569In Stock
1 mL x 10 mM (in DMSO)$54In Stock
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Product Introduction

Bioactivity
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.
Targets&IC50
ERR:3.3 nM
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]
Kinase Assay
Cytosol (200 μL) is incubated for 30 min at 4°C with different concentrations of oestradiol, tamoxifen and (4-Hydroxytamoxifen) or dihydroxytamoxifen administered in 10 μL methanol. Control tubes are incubated with 10 μL methanol alone and non-specific binding is determined in a parallel incubation of cytosol (200 μL) with methanol (10 μL) containing DES (5 × 106 M). [2,4,6,7-3H]Oestradiol solution (50 μL) in TED buffer is added to each tube to give a final concentration of 2 × 10-9 M. Incubation is continued for 4 h (4°C) and then 400 μL of a suspension of dextran-coated charcoal (250 mg % Norit A, 2.5 mg % dextran) in TED buffer is added and allowed to stand for 20 min. Tubes are centrifuged at 800 g for 10 min (4°C) and 400 μL samples of the supernatant are added to 10 mL tritium scintillator (6 g butyl PBD, 135 mL toluene, 720 ml dioxane, 100 g naphthalene, 45 mL absolute methanol). Samples are counted for 10 min in a liquid scintillation spectrometer. Counting efficiency is determined by external standardization (35-36 %). Results are represented as a percentage of the specifically bound radioactivity (c.p.m.) in the control tubes[1].
Animal Research
4-Hydroxytamoxifen is formulated in sesame oil[3].Animals of each sex are divided into two groups: one group receives 4-Hydroxytamoxifen [6 μg/0.1 mL sesame oil/day, subcutaneously (s.c.) starting at 06.00 h] injections for three consecutive days, while the other group receives an equivalent amount of sesame oil injection for 3 days. Four hours following the third injection, each group is then subdivided into two groups: one receives four cumulative doses of methamphetamine hydrochloride (10 mg/kg, s.c.), and the other receives a comparable volume of saline at 2-h intervals. Bilateral gonadectomy is performed under pentobarbital anesthesia (50 mg/kg, intraperitoneally). Five weeks after surgery, gonadectomized mice of each sex are randomly divided into six groups. Five groups of each sex receive three daily injections of various concentrations of 4-Hydroxytamoxifen (0, 1.5, 3.0, 6.0, and 12.0 μg/0.1 mL sesame oil/day). Four hours following the third injection, mice receive four doses of methamphetamine (MA, 10 mg/kg) at 2-h intervals. The remaining group of each sex receives sesame oil pretreatment for three consecutive days, followed by saline injections, and serves as the control group[3].
AliasICI 79280, (Z)-4-hydroxy Tamoxifen, trans-4-Hydroxytamoxifen
Chemical Properties
Molecular Weight387.51
FormulaC26H29NO2
Cas No.68047-06-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 0.1 mg/mL (insoluble)
DMSO: 45 mg/mL (116.13 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5806 mL12.9029 mL25.8058 mL129.0289 mL
5 mM0.5161 mL2.5806 mL5.1612 mL25.8058 mL
10 mM0.2581 mL1.2903 mL2.5806 mL12.9029 mL
20 mM0.1290 mL0.6451 mL1.2903 mL6.4514 mL
50 mM0.0516 mL0.2581 mL0.5161 mL2.5806 mL
100 mM0.0258 mL0.1290 mL0.2581 mL1.2903 mL

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