Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LSZ-102是一种有效和选择性的雌激素受体降解剂(IC50 = 0.2 nM),可用于有关ERα阳性乳腺癌的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 996 | 现货 | ||
2 mg | ¥ 1,470 | 现货 | ||
5 mg | ¥ 2,420 | 现货 | ||
10 mg | ¥ 3,990 | 现货 | ||
25 mg | ¥ 6,390 | 现货 | ||
50 mg | ¥ 8,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,510 | 现货 |
产品描述 | LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer. |
体外活性 | LSZ-102 causes significant degradation of ERα after 24 h when given as a 10 μM solution to MCF-7 cells. LSZ-102 currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. Robust inhibition of cell proliferation in MCF-7 cells is observed upon incubation with LSZ-102 with a half inhibitory concentration of 1.7 nM. Results show that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 (IC50: 0.3 nM)[1]. |
体内活性 | In male Sprague-Dawley rats, LSZ-102 (3 mg/kg) causes 33% bioavailability and a dose-normalized exposure of 620 nM•h. In mice, LSZ-102 (20 mg/kg) causes significant tumor growth inhibition resulting in tumor stasis[1]. |
别名 | LSZ102 |
分子量 | 470.46 |
分子式 | C25H17F3O4S |
CAS No. | 2135600-76-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (191.3 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 | 2.1256 mL | 10.6279 mL | 21.2558 mL | 53.1395 mL |
5 mM | 0.4251 mL | 2.1256 mL | 4.2512 mL | 10.6279 mL | |
10 mM | 0.2126 mL | 1.0628 mL | 2.1256 mL | 5.3139 mL | |
20 mM | 0.1063 mL | 0.5314 mL | 1.0628 mL | 2.657 mL | |
50 mM | 0.0425 mL | 0.2126 mL | 0.4251 mL | 1.0628 mL | |
100 mM | 0.0213 mL | 0.1063 mL | 0.2126 mL | 0.5314 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。
LSZ-102 2135600-76-7 Endocrinology/Hormones Estrogen Receptor/ERR LSZ 102 LSZ102 Inhibitor inhibitor inhibit