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Topotecan

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产品价格:电议      采购度:1590      原产地:美洲

发布时间:2021/7/27 1:02:07      所属地区:上海 上海市

简要描述:

Topotecan (SKF 104864A; NSC 609669) 是拓扑异构酶I抑制剂。

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Topotecan

CAS No. : 123948-87-8

MCE 站:Topotecan

产品活性:Topotecan (SKF 104864A; NSC 609669) 是拓扑异构酶I抑制剂。

研究领域:Cell Cycle/DNA Damage  |  Autophagy

作用靶点:Topoisomerase  |  Autophagy

In Vitro: Topotecan (SKF104864) obviously inhibits proliferation of not only human glioma cells but also glioma stem cells (GSCs) in a dose- and time-dependent manner. According to the IC50 values at 24 h, 3 μM of Topotecan (SKF104864) is selected as the optimal administration concentration. In addition, Topotecan (SKF104864) induces cell cycle arrest in G0/G1 and S phases and promoted apoptosis. Results show that the cell viability is inhibited by Topotecan (SKF104864) in a dose-dependent manner. 2, 20 and 40 μM of Topotecan obviously inhibits the cell viability compared with the control groups. The IC50 values of Topotecan (SKF104864) at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87. Thus 3 μM of Topotecan is selected as the optimal administration concentration in the subsequent experiments.

In Vivo: NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days treatment. Compared with the control, Low dose metronomic (LDM) Topotecan (TP) and TP+Pazopanib (PZ) liver weights are significantly lower in TP+PZ-treated animals, compared with PZ. Microscopic tumors are visible in the livers of mice belonging to all the groups except TP+PZ confirming the ability of TP+PZ to control liver metastasis. In a previous dose-response study, the daily dose of oral metronomic Topotecan (0.5, 1.0, and 1.5 mg/kg) causes greater reduction in microvascular density compared with weekly maximum-tolerated dose regimen (7.5 and 15 mg/kg) in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan show decreased food intake, and a lesser antitumor effect.

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更新时间:2024/1/2 10:16:09

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