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Topoisomerase I/II inhibitor 3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Topoisomerase I/II inhibitor 3图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Topoisomerase I/II inhibitor 3 (7) 是一种有效的拓扑异构酶 I (Topo I)II (Topo II)双抑制剂。Topoisomerase I/II inhibitor 3 通过抑制PI3K/Akt/mTOR 信号通路抑制细胞增殖、侵袭和迁移,诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 可用于肝癌的研究。
生物活性

TopoisomeraseI/II inhibitor 3 (compound 7) is a potenttopoisomeraseI (Topo I)andII (Topo II)dual inhibitor.TopoisomeraseI/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induceapoptosisby inhibitingPI3K/Akt/mTOR signaling pathway.TopoisomeraseI/II inhibitor 3 can be used for livercancerresearch[1].

IC50& Target

Topoisomerase I

 

Topoisomerase II

 

PI3K

 

体外研究
(In Vitro)

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 IC50values 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.
体内研究
(In Vivo)

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 LD50between 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 LD50between 250 and 400 mg/kg.
分子量

404.46

Formula

C24H24N2O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.