Topotecan拓扑替康,123948-87-8

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Topotecan

CAS No. : 123948-87-8

MCE 国际站：Topotecan

产品活性：Topotecan (SKF 104864; NSC 609669) 是一种口服有效的拓扑异构酶 I (Topoisomerase I) 抑制剂。Topotecan 诱导细胞周期阻滞在 G0/G1 和 S 期，促进凋亡 (apoptosis)。Topotecan 具有抗癌活性。

研究领域：Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

作用靶点：Topoisomerase  |  Autophagy  |  Apoptosis

In Vitro: Topotecan obviously inhibits proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner.
Topotecan (0-40 μM) obviously inhibits the cell viability compared with the control groups, in a dose-dependent manner.
Topotecan shows anti-proliferation activity against U251, U87, GSCs-U251 and GSCs-U87 cells, with IC₅₀ values of 2.73±0.25, 2.95±0.23, 5.46±0.41, and 5.95±0.24 μM, respectively.

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.
Topotecan (0.5, 1.0, and 1.5 mg/kg; Orally, daily) causes greater reduction in microvascular density 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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