Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 10-14周 | ||
50 mg | ¥ 13,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
产品描述 | Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1]. |
体外活性 | Topoisomerase IIα-IN-4 (0-50 μM; 72 h) shows antiproliferative activities against cancer cells [1]. Topoisomerase IIα-IN-4 shows high inhibitory activity and subtypeselectivity against TopoIIα and β with IC 50 s of 3.8 and 10.1 μM, respectively [1]. Topoisomerase IIα-IN-4 (0.3 μM; 4 h) is a non-intercalative TopoIIα catalytic inhibitor [1]. Topoisomerase IIα-IN-4 (0.5-1 μM; 48 h) induces cell apoptosis [1]. Topoisomerase IIα-IN-4 (0.5-1 μM; 24 h) induces cell-cycle arrest [1]. Cell Proliferation Assay [1] Cell Line: HeLa, HCT-116, MDA-MB231, HepG2, A549, CCL-226, BEAS-2B and HL-7702 cell lines Concentration: 0-50 μM Incubation Time: 72 hours Result: Inhibited HeLa, HCT-116, MDA-MB 231, HepG2, A549, CCL-226, BEAS-2B and HL-7702 cells with IC 50 s of 0.1, 0.2, 0.3, 0.2, 0.3, 0.3, >50, 31.9 and 16.7 μM, respectively. Western Blot Analysis [1] Cell Line: HepG-2 cell line Concentration: 0.3 μM Incubation Time: 4 hours Result: Showed no effect on the level of phospho-histone H2AX. Apoptosis Analysis [1] Cell Line: 0.5-1 μM Concentration: 0.3 μM Incubation Time: 48 hours Result: Increased the total numbers of early and late apoptotic cells from 6.0% to 70.6% at the concentration of 1 μM. |
体内活性 | Topoisomerase IIα-IN-4 (500 mg/kg; p.o. twice at the first day) shows no acute toxicity in vivo [1]. Animal Model: C57BL/6 mice [1] Dosage: 500 mg/kg Administration: Oral gavage; 500 mg/kg twice at the first day Result: Exerted lower toxicity in this established test and caused no significant difference of body weight of mice. |
分子量 | 367.44 |
分子式 | C25H21NO2 |
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。
Topoisomerase IIα-IN-4 Inhibitor inhibitor inhibit