4-羟基他莫昔芬 T4420

Product Introduction
Bioactivity


英文名: 4-Hydroxytamoxifen

描述: 4-Hydroxytamoxifen (ICI 79280) 是 Tamoxifen 的活性代谢产物，是一种雌激素受体调节剂 (SERM)，具有选择性和口服有效性。4-Hydroxytamoxifen 具有抗肿瘤活性，可用于乳腺癌的研究。

激酶实验: 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].

动物实验: 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].

体外活性: 方法：人子宫内膜腺癌细胞系 HEC-1B 用 4-Hydroxytamoxifen (0.01-100 µM) 处理 3 天，使用 CellTiter 96 AQueous One Solution Cell Proliferation Assay 检测细胞活力。结果：暴露于更高浓度 (1-100 µM) 的 4-Hydroxytamoxifen 的 HEC-1B 细胞显示出不同浓度之间细胞存活率的显著差异。[1]方法：ER-阳性乳腺癌症细胞系 MCF-7、T47D 和 BT-474 用 4-Hydroxytamoxifen (0.5-1 µM) 和 sulforaphane (5 µM) 处理 48 h，使用 Western Blot 检测靶点蛋白表达水平。结果：Sulforaphane 诱导 PARP 切割，其强度取决于细胞系。sulforaphane 和 4-Hydroxytamoxifen 的联合治疗进一步提高了 PARP 的切割。[2]

体内活性: 方法：为检测体内抗肿瘤活性，将 Cholesterol (1 mg/kg) 腹腔注射给携带人乳腺癌肿瘤 MCF-7 的 Nu/Nu 小鼠，每天一次，持续二十三天。结果：4-Hydroxytamoxifen 有效地抑制小鼠的肿瘤生长。[3]方法：为诱导 Cre 重组酶活性，将 Cholesterol (30-60 mg/kg) 腹腔注射给 Rosa26BEST1-CreERT2 小鼠，每天一次，持续四天。结果：TdTomato 在两性小鼠的 RPE 中强烈表达。[4]

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

溶解度: H2O : < 0.1 mg/mL (insoluble)
DMSO : 28 mg/mL (72.26 mM)


关键字: 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

相关产品: Segetalin B | Endoxifen | GLL 398 | FLTX1 | Nafoxidine | DY131 | AZD9496 | Delphinidin chloride | (±)-Equol | Giredestrant tartrate

相关库: ReFRAME Related Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Active Compound Library | Endocrinology-Hormone Compound Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途