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Topoisomerase I inhibitor 5

CAS No. : 2513461-95-3

MCE 站：Topoisomerase I inhibitor 5

产品活性：Topoisomerase I inhibitor 5 是一种有效的拓扑异构酶 (topoisomerase) 抑制剂。Topoisomerase I inhibitor 5 能干扰 DNA，显著抑制 Topoisomerase I 活性。Topoisomerase I inhibitor 5 能将细胞周期阻滞在 G1 期，诱导 MCF-7 细胞凋亡 (apoptosis)。Topoisomerase I inhibitor 5 具有逆转 P-gp 介导的阿霉素耐药性的效力。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：Topoisomerase  |  DNA/RNA Synthesis  |  Apoptosis

In Vitro: Topoisomerase I inhibitor 5 (compound 14) (0-50 μM; 48 hours) exhibits antiproliferation activity against cancer cell lines ａnd lower cytotoxicity in normal cells.
Topoisomerase I inhibitor 5 (2-8 μM; 24 hours) induces MCF-7 cell cycle arrest at the G1 phase.
Topoisomerase I inhibitor 5 (2-8 μM; 48 hours) increases the apoptotic rate of MCF-7/ADR ａnd MCF-7 cells.
Topoisomerase I inhibitor 5 (1.5-6 μM; 24 hours) increases the expression degree of cleaved-caspase-3 ａnd cleaved-PARP in MCF-7; down-regulates the level of anti-apoptotic protein, up-regulates the levels of pro-apoptotic proteins in MCF-7/ADR.
Topoisomerase I inhibitor 5 (0.1 μM; 24 hours) induces cell apoptosis by promoting the accumulation of ROS in MCF-7/ADR cell.
Topoisomerase I inhibitor 5 (10 μg/ml; 24 hours) increases the accumulation of the ADR ａnd Rh123 in MCF-7/ADR cells.
Topoisomerase I inhibitor 5 (5, 10 ａnd 20 μM; 24 hours) reduces the expression degree of P-gp by 14.95% ａnd 18.10% in MCF-7/ADR cells at 10 ａnd 20 μM.

In Vivo: Topoisomerase I inhibitor 5 (1 mg/kg ａnd 10 mg/kg; IV; every two days, for 21 days) decreases the tumor growth significantly.

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