Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 997 | 现货 | ||
5 mg | ¥ 2,630 | 现货 | ||
10 mg | ¥ 3,930 | 现货 | ||
25 mg | ¥ 6,320 | 现货 | ||
50 mg | ¥ 8,660 | 现货 | ||
100 mg | ¥ 11,600 | 现货 | ||
500 mg | ¥ 23,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,920 | 现货 |
产品描述 | FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus. |
靶点活性 | ERα:87.5 nM |
体外活性 | Competition studies showed that FLTX1 binding was totally displaced by unlabeled tamoxifen and partially by estradiol, indicating the existence of non-ER-related triphenylethylene-binding sites.?Ligand binding assays showed that FLTX1 exhibits similar affinity for ER than tamoxifen.?FLTX1 exhibited antiestrogenic activity comparable to tamoxifen in MCF7 and T47D cells transfected with 3xERE-luciferase reporter.?FLTX1 lacked the strong agonistic effect of tamoxifen on ERα-dependent transcriptional activity[1]. |
体内活性 | In vivo assays in mice revealed that unlike tamoxifen, FLTX1 was devoid of estrogenic uterotrophic effects, lacked of hyperplasic and hypertrophic effects, and failed to alter basal proliferating cell nuclear antigen immunoreactivity.?In the rat uterine model of estrogenicity/antiestrogenicity, FLTX1 displayed antagonistic activity comparable to tamoxifen at lower doses, and only estrogenic uterotrophy at the highest dose[2]. |
分子量 | 520.58 |
分子式 | C31H28N4O4 |
CAS No. | 1481401-71-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.21 mg/mL (10 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9209 mL | 9.6047 mL | 19.2093 mL | 48.0234 mL |
5 mM | 0.3842 mL | 1.9209 mL | 3.8419 mL | 9.6047 mL | |
10 mM | 0.1921 mL | 0.9605 mL | 1.9209 mL | 4.8023 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。
FLTX1 1481401-71-1 Endocrinology/Hormones Estrogen Receptor/ERR Estrogen/progestogen Receptor cancer Inhibitor fluorescent Tamoxifen antiestrogenic inhibit non-permeabilized receptor breast FLTX 1 estrogen permeabilized FLTX-1 uterus inhibitor