Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Topoisomerase I/II inhibitor 3 (化合物7) 是拓扑异构酶 I (Topo I)和 II (Topo II)的有效双抑制剂。 通过抑制 PI3K/Akt/mTOR 信号通路,Topoisomerase I/II inhibitor 3抑制细胞增殖、侵袭和迁移,诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 在肝癌中具有研究价值。
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 I/II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) . By inhibiting PI3K /Akt/mTOR signaling pathway, Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis . Topoisomerase I/II inhibitor 3 has research value in liver cancer. |
体外活性 | Topoisomerase I/II inhibitor 3 (compound 7) (0-100 μM) can insert into DNA and change the topology of DNA, cause DNA damage to a certain extent [1]. Topoisomerase I/II inhibitor 3 (0-4 μM, 24 h) inhibits HCC (hepatocellular carcinoma) cells proliferation in a dose-dependent manner, inhibits migration and invasion of LM9 and HuH7 cells by inhibiting the expression of MMP-9 [1]. Topoisomerase I/II inhibitor 3 (0-14 μM, 48 h) significantly induces the apoptosis of LM9 and HuH7 cells, and induces mitochondrial dysfunction and ROS burst in a dose-dependent manner [1]. Topoisomerase I/II inhibitor 3 (0-7 μM, 48 h) reduces the expression of the inhibitory factor Bcl-2 and promotes the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibits the phosphorylation of PI3K/Akt/mTOR signaling pathway [1]. Cell Proliferation Assay Cell Line: HCC cells (HuH7 and LM9) [1] Concentration: 0, 0.5, 1, 2, and 4 μM Incubation Time: 24 h Result: Inhibited HCC cells proliferation in a dose-dependent manner, with IC 50 values of 2.10 μM (LM9) and 1.93 μM (HuH7), respectively, and dose-dependently inhibited the formation of cell colonies. Apoptosis Analysis Cell Line: LM9 and HuH7 cells [1] Concentration: 0, 1.8, 3.5, 7, and 14 μM Incubation Time: 48 h Result: Significantly induced the apoptosis of LM9 and HuH7 cells in a concentration-dependent manner. Western Blot Analysis Cell Line: LM9 and HuH7 cells [1] Concentration: 0, 1.8, 3.5, and 7 μM Incubation Time: 48 h Result: Reduced the expression of the inhibitory factor Bcl-2 and promoted the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibited the phosphorylation of PI3K/Akt/mTOR signaling pathway. |
体内活性 | Topoisomerase I/II inhibitor 3 (compound 7) (male Kunming mice, 0-400 mg/kg, IP, once) causes the mice in the 400 mg/kg group die, with the LD 50 between 250 and 400 mg/kg [1]. Animal Model: Male Kunming mice (19-22 mg, 8 mice, 4 groups) [1] Dosage: 200, 250, 400 mg/kg (dissolved in 5% DMSO and castor oil) Administration: IP, once Result: Did not cause the mice in the 250 mg/kg and 200 mg/kg groups die after 2 weeks of administration, and caused the mice in the 400 mg/kg group die, with the LD 50 between 250 and 400 mg/kg. |
分子量 | 404.46 |
分子式 | C24H24N2O4 |
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 I/II inhibitor 3 Inhibitor inhibitor inhibit