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Tamoxifen Citrate 是一种口服有效的,选择性雌激素受体调节剂,可阻断乳腺细胞中的雌激素作用,并可激活如骨骼、肝脏和子宫细胞中的雌激素活性。它是 Hsp90激活剂,可增强 Hsp90 分子伴侣 ATPase 的活性,可激活自噬和诱导凋亡。
Tamoxifen Citrate 是一种口服有效的,选择性雌激素受体调节剂,可阻断乳腺细胞中的雌激素作用,并可激活如骨骼、肝脏和子宫细胞中的雌激素活性。它是 Hsp90激活剂,可增强 Hsp90 分子伴侣 ATPase 的活性,可激活自噬和诱导凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | ¥ 108 | 现货 | |
500 mg | ¥ 229 | 现货 | |
1 g | ¥ 329 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 239 | 现货 |
产品描述 | Tamoxifen is an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). |
体外活性 | Tamoxifen因其抗雌激素活性(ER)显现出抗肿瘤效果。Tamoxifen对ER的表观亲和力值根据不同ER来源(物种)、蛋白浓度和测定条件。Tamoxifen诱导程序性细胞死亡。[1]Tamoxifen在MCF-7细胞上抑制[3H]胸腺嘧啶掺入和DNA聚合酶活性,并减少培养物中的DNA含量和细胞数量。通过添加雌二醇到培养基中可以迅速逆转Tamoxifen对MCF-7细胞生长的抑制效果。2和6μM Tamoxifen可减少处于S期的细胞比例,增加G1期的细胞数量。在10μM时,Tamoxifen在48小时内引起细胞死亡。[2]Tamoxifen在10天治疗后以约10nM的IC50抑制MCF-7生长。Tamoxifen抑制MCF-7的纤溶酶原激活剂活性,并抑制雌二醇刺激的纤溶酶原激活剂活性。Tamoxifen还引起细胞孕酮受体水平小幅度增加。[3]Tamoxifen能够抑制前列腺癌细胞PC3,PC3-M和DU145的生长(IC50范围为5.5-10μM),这与其抑制蛋白激酶C和诱导p21(waf1/cip1)的表达有关。[4] |
体内活性 | 在快速生长的雌二醇刺激的MCF-7异种移植瘤之中,Tamoxifen的施用会引起剂量依赖性的肿瘤生长延缓或停滞,显著降低肿瘤细胞在瘤内的增殖。与未经治疗、体积加倍时间为5天、Tpot为2.3天、及%LI为23%的小鼠相比,经Tamoxifen处理的细胞在肿瘤生长放缓(肿瘤加倍时间,12天)、肿瘤潜在加倍时间(Tpot)显著增长(达6.6天)和标记指数(%LI)至第23天后下降至8%。[5] Tamoxifen不仅具有抗雌激素作用,还依赖于物种、组织和基因表现出雌激素特性。它在骨骼和血清脂质浓度方面表现出有利影响,对子宫内膜有促激作用。[1] |
激酶实验 | Competitive binding assays: Cells are harvested from 150-sq cm T-flasks, and cytosol is prepared at a protein concentration of approximately 2 mg/mL in phosphate buffer. Aliquots of this 180,000 ×g supernatant are then incubated with various concentrations of Tamoxifen and 2.5 nM [3H]estradiol for 16 hr at 0-4 ℃. The free steroids are absorbed by dextran-charcoal [l0 μL of 0.5% Dextran C-5% Norite A in TE buffer] for 1 hr at 0 ℃, and aliquots are counted after centrifugation at 800 ×g, 30 min. The relative binding ability of each competitor is taken as the ratio of the concentration of radioinert estradiol/competitor required to inhibit one-half of the specific [3H]estradiol binding, with the affinity of estradiol set at 100%. |
细胞实验 | MCF-7 cells are seeded into T-25 flasks (1.5×105 cells/flask) and grown for 2 days in the MEM supplemented with 10 mM HEPES buffer, gentamicin (50 μg/mL), penicillin (100 units/mL), streptomycin (0.1 mg/mL), bovine insulin (6 ng/mL), hydrocortisone (3.75 ng/mL), and 5% calf serum that has been treated with dextran-coated charcoal for 45 min at 55 ℃ to remove endogenous hormones. The medium is then changed to MEM supplemented as described above, except that it contains 2% charcoal dextran-treated calf serum and various concentrations of Tamoxifen. At the end of incubation, cell numbers are counted. (Only for Reference) |
别名 | 他莫昔芬柠檬酸盐, 枸橼酸他莫昔芬, Tamoxifen Z-isomer citrate, ICI 46474 Citrate, ICI 46474 |
分子量 | 563.65 |
分子式 | C32H37NO8 |
CAS No. | 54965-24-1 |
Smiles | CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1.C(C(=O)O)C(CC(=O)O)(C(=O)O)O |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (88.71 mM), Sonication is recommended. Ethanol: 2.8 mg/mL (5 mM)), Heating is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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