Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity. 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 Epertinib hydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,500 | 6-8周 | ||
50 mg | ¥ 13,700 | 6-8周 | ||
100 mg | ¥ 17,400 | 6-8周 |
Epertinib 的其他形式现货产品:
产品描述 | Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity. |
靶点活性 | EGFR:1.48 nM, HER2:2.49 nM, HER4:7.15 nM |
体外活性 | Epertinib displays inhibitory activity against the growth of cancer cell lines expressing EGFR and/or HER2 (IC50s: 8.3 nM (NCI-N87 (stomach)), 9.9 nM (BT-474 (breast)), and 14 nM (SK-BR-3 (breast))) [1]. Epertinib shows no effect on KDR, IGF1R, SRC, KIT, and PDGFRβ (IC50, >10000 nM). Epertinib inhibits relative phosphorylation of EGFR and HER2 in NCI-N87 cells (IC50s: 4.5 and 1.6 nM) and it also inhibits MDA-MB-361 cell growth (IC50: 26.5 nM) [2]. |
体内活性 | Epertinib displays antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days ( ED50:10.2 mg/kg). Epertinib (50 mg/kg, p.o.) is four times more potent activity than GW572016 and completely inhibits the growth of cancer cells in mice [1] and it also obviously decreases the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model [2]. |
别名 | S-22611 |
分子量 | 560.02 |
分子式 | C30H27ClFN5O3 |
CAS No. | 908305-13-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Epertinib 908305-13-5 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER S 22611 S-22611 S22611 Inhibitor inhibitor inhibit