4-Hydroxytamoxifen NEW
| Price | $64 | $89 | $197 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-12 |
Product Details
| Product Name: 4-Hydroxytamoxifen | CAS No.: 68047-06-3 |
| Purity: 99.84% | Supply Ability: 10g |
| Release date: 2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | 4-Hydroxytamoxifen |
| 描述 | 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. |
| 激酶實(shí)驗(yàn) | 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]. |
| 動(dòng)物實(shí)驗(yàn) | 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]. |
| 體外活性 | 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] |
| 體內(nèi)活性 | 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] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 0.1 mg/mL (insoluble) DMSO : 45 mg/mL (116.13 mM) |
| 關(guān)鍵字 | inhibit | Estrogen Receptor/ERR | 4-hydroxy Tamoxifen | estrogen receptor | oral | CRISPR/Cas9 | ICI79280 | 4-Hydroxytamoxifen | 4Hydroxytamoxifen | Inhibitor | (Z)-Afimoxifene | nucleus translocation | 4 Hydroxytamoxifen | ICI-79280 |
| 相關(guān)產(chǎn)品 | Kaempferol | Mifepristone | Estradiol | Astragaloside IV | Cholesterol | Melatonin | Ethisterone |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | ReFRAME 相關(guān)化合物庫 | 抗卵巢癌化合物庫 | 內(nèi)分泌激素分子庫 | NO PAINS 化合物庫 | 口服活性化合物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 人代謝物化合物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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