分子式：C26H29NO·C6H8O7 分子量：563.64
产品简介：枸橼酸他莫昔芬结构与雌激素相似，它可以与核内雌激素受体(En)竞争结合，形成受体复合物，抑制细胞分裂、生长，阻止雌激素发挥作用。
物理性状及指标：
外观：……………………白色或类白色粉末
溶解性：…………………DMSO: 20 mg/mL
含量：……………………>99.0%
生物活性 : (来自公开文献，仅供参考)
| 靶点 | Estrogen receptor |
| 体外研究 | Effects of tamoxifen citrate on cell growth of MCF-7, UM-SCC-5, and UM-SCC-17B. Cells were used during passages (P) 202, 66, and 46, respectively. Three days after plating, cells were treated with tamoxifen citrate at concentrations of 1, 2, 3, 4, 5, 6, 7, or 8 µ /L, as indicated. Cultures were fed daily with complete Eagle’s minimum essential medium supplemented with 5% dextran 70-charcoal-treated fetal bovine serum (D5). Drug solutions were prepared fresh for each feeding, and controls were fed with D5 containing 0.07% alcohol. Replicate wells were harvested by trypsin-edetic acid, and viable cells were counted and plotted as average cell number per well[1]. |
| 体内研究 | SB pre-treatment group: animals were divided into three subgroups (7 rats/group): Subgroup I (SB-1): rats received SB for 7 days and then received saline for 14 days. Subgroup II (TC-1): rats received saline for 7 days and then received TC for 14 days. Subgroup III (SB-TC): rats received SB for 7 days and then received TC for 14 days. SB post-treatment group: animals of this group were divided into three subgroups (7 rats/group): Subgroup I (SB-2): rats received saline for 14 days and then received SB for 7 days. Subgroup II (TC-2): rats received TC for 14 days and then received saline for 7 days. Subgroup III (TC-SB): rats received TC for 14 days and then received SB for 7 days[2]. |
| 参考文献 | [1]:Growth Inhibition of Laryngeal UM-SCC Cell Lines by Tamoxifen: Comparison With Effects on the MCF-7 Breast Cancer Cell Line | JAMA Otolaryngology–Head & Neck Surgery | JAMA Network. [2]:Potential anti-genotoxic effect of sodium butyrate to modulate induction of DNA damage by tamoxifen citrate in rat bone marrow cells | SpringerLink |
用途及描述：科研试剂，广泛应用于分子生物学，药理学等科研方面，严禁用于人体；
- 产生持久的抗雌激素效应，是乳腺癌术后辅助内分泌治疗的首选药物；
- 临床用于治疗女性复发转移乳腺癌和手术后转移的辅助治疗，预防复发；
- 枸橼酸他莫昔芬可以通过降低膜流通性和增强细胞间结合部位的刚性, 使癌症转移促进剂及各种活化酶浓度和活性减少，从而抑制或阻碍癌细胞的生长和转移；
- 它还可以促使肿瘤病灶周围细胞分泌负性生长因子—转化生长因子TGF—G，扼制癌细胞的无限繁殖；
- 并可抑制由人体中性白细胞所产生的过氧化氢造成DNA 碱基发生氧化性破坏，故其对于乳腺癌之外的其他恶性肿癌的治疗和预防均有益处。
储存条件：常温，避光防潮密闭干燥。