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4-Hydroxytamoxifen

Catalog No. T4420 CAS 68047-06-3

Synonyms: ICI 79280, (Z)-4-hydroxy Tamoxifen, trans-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.

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4-Hydroxytamoxifen, CAS 68047-06-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 64.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 386.00
100 mg	In stock	$ 569.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.84%

Purity: 99.56%

Purity: 99.37%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Synonyms	ICI 79280, (Z)-4-hydroxy Tamoxifen, trans-4-Hydroxytamoxifen
Molecular Weight	387.51
Formula	C26H29NO2
CAS No.	68047-06-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 28 mg/mL (72.26 mM)

References and Literature

1. Cuevas ME, et al. In vitro cytotoxicity of 4'-OH-tamoxifen and estradiol in human endometrial adenocarcinoma cells HEC-1A and HEC-1B. Oncol Rep. 2015 Jan;33(1):464-70. 2. Pawlik A, et al. Sensitization of estrogen receptor-positive breast cancer cell lines to 4-hydroxytamoxifen by isothiocyanates present in cruciferous plants. Eur J Nutr. 2016 Apr;55(3):1165-80. 3. Zhong Q, et al. Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status. BMC Cancer. 2015 Sep 9;15:625. 4. Chen M, et al. An efficient inducible RPE-Selective cre transgenic mouse line. Exp Eye Res. 2021 Jan;202:108370.

Citations

1. Lu Y, Yang Q, Su Y, et al. MYCN mediates TFRC-dependent ferroptosis and reveals vulnerabilities in neuroblastoma. Cell Death & Disease. 2021, 12(6): 1-14.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Ovarian Cancer Compound Library Endocrinology-Hormone Compound Library Orally Active Compound Library NO PAINS Compound Library ReFRAME Related Library Human Metabolite Library Immunology/Inflammation Compound Library

Related Products

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CIDD-0149897 Etonogestrel Estrogen receptor modulator 8 (E/Z)-4-Hydroxytamoxifen Liquiritigenin Diethylstilbestrol G36 Isopsoralenoside

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Keywords

4-Hydroxytamoxifen 68047-06-3 Endocrinology/Hormones Estrogen Receptor/ERR Estrogen/progestogen Receptor inhibit 4-hydroxy Tamoxifen estrogen receptor oral ICI 79280 CRISPR/Cas9 ICI79280 (Z)-4-hydroxy Tamoxifen 4Hydroxytamoxifen Inhibitor trans-4-Hydroxytamoxifen (Z)-Afimoxifene nucleus translocation 4 Hydroxytamoxifen ICI-79280 inhibitor

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