Name: Tamoxifen Citrate
Brand: TargetMol
SKU: T0835
Price: 108 CNY
Availability: InStock
Rating: 5 (10 reviews)

Tamoxifen Citrate

很棒

产品编号 T0835Cas号 54965-24-1

别名 他莫昔芬柠檬酸盐, 枸橼酸他莫昔芬, Tamoxifen Z-isomer citrate, ICI 46474 Citrate

Tamoxifen Citrate 是一种口服有效的选择性雌激素受体调节剂（SERM），可阻断乳腺细胞中的雌激素作用，同时激活骨骼、肝脏和子宫等细胞中的雌激素活性，作为Hsp90激活剂可增强其分子伴侣ATPase活性，能激活自噬、诱导凋亡，并可用于构建CreER(T2)转基因小鼠的基因敲除及肝损伤模型。

规格

价格

库存

数量

100 mg

¥ 108

In stock

500 mg

¥ 229

In stock

1 g

¥ 329

In stock

1 mL x 10 mM (in DMSO)

¥ 239

In stock

产品介绍

生物活性

产品描述	Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.
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

化学信息

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
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7742 mL	8.8708 mL	17.7415 mL	88.7075 mL
5 mM	0.3548 mL	1.7742 mL	3.5483 mL	17.7415 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.1774 mL	0.8871 mL	1.7742 mL	8.8708 mL
20 mM	0.0887 mL	0.4435 mL	0.8871 mL	4.4354 mL
50 mM	0.0355 mL	0.1774 mL	0.3548 mL	1.7742 mL

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是 10 mg/kg ，每只动物体重 20 g ，给药体积 100 μL ， TargetMol | Animal experiments

一共给药动物 10 只 ，您使用的配方为 5% TargetMol | reagent

DMSO+ 30%PEG300+ 5%Tween 80 + 60%Saline/PBS/ddH₂O，那么您的工作液浓度为 2 mg/mL 。

母液配置方法: 2 mg 药物溶于 50 μLDMSO TargetMol | reagent

（母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法: 取 50μLDMSO TargetMol | reagent

母液，添加 300 μLPEG300 TargetMol | reagent

混匀澄清，再加 50μLTween 80, 混匀澄清，再加 600μLSaline/PBS/ddH₂O TargetMol | reagent

混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

Tamoxifen Citrate

Tamoxifen Citrate

产品介绍

计算器

体内实验配液计算器

剂量转换

SCI 文献

关键词

评论列表