Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Endoxifen Z-isomer hydrochloride (Endoxifen HCl) 是Tamoxifen 最重要的代谢产物, 在表达ERα的乳腺癌细胞中发挥抗雌激素作用, Endoxifen HCl 以浓度依赖的方式抑制hERG, IC50值为1.6μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 420 | 5日内发货 |
Endoxifen Z-isomer hydrochloride 的其他形式现货产品:
产品描述 | Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist. |
靶点活性 | ERG (human):1.6 μM |
体外活性 | Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5] |
体内活性 | In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3] |
细胞实验 | MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.(Only for Reference) |
别名 | Endoxifen HCl, Z-因多昔芬盐酸盐 |
分子量 | 409.95 |
分子式 | C25H28ClNO2 |
CAS No. | 1032008-74-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: <1 mg/mL
Ethanol: 69 mg/mL (168.3 mM)
DMSO: 69 mg/mL (168.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.4393 mL | 12.1966 mL | 24.3932 mL | 60.983 mL |
5 mM | 0.4879 mL | 2.4393 mL | 4.8786 mL | 12.1966 mL | |
10 mM | 0.2439 mL | 1.2197 mL | 2.4393 mL | 6.0983 mL | |
20 mM | 0.122 mL | 0.6098 mL | 1.2197 mL | 3.0492 mL | |
50 mM | 0.0488 mL | 0.2439 mL | 0.4879 mL | 1.2197 mL | |
100 mM | 0.0244 mL | 0.122 mL | 0.2439 mL | 0.6098 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% 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 μL DMSO (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 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Endoxifen Z-isomer hydrochloride 1032008-74-4 Angiogenesis Endocrinology/Hormones JAK/STAT signaling Membrane transporter/Ion channel Tyrosine Kinase/Adaptors Estrogen/progestogen Receptor Potassium Channel HER Estrogen Receptor/ERR inhibit Inhibitor Endoxifen Z-isomer Hydrochloride Endoxifen HCl Z-因多昔芬盐酸盐 KcsA Endoxifen Z-isomer Endoxifen Z isomer hydrochloride Endoxifen Zisomer hydrochloride inhibitor