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Topoisomerase I inhibitor 5

Catalog No. T61501 CAS 2513461-95-3

Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].

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Topoisomerase I inhibitor 5 Chemical Structure

Topoisomerase I inhibitor 5, CAS 2513461-95-3

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 2,140.00
50 mg	6-8 weeks	$ 2,785.00
100 mg	6-8 weeks	$ 3,520.00

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Description	Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].
In vitro	Topoisomerase I inhibitor 5 (compound 14) demonstrates significant antiproliferative effects against various cancer cell lines at concentrations ranging from 0 to 50 μM over 48 hours, while exhibiting lower cytotoxicity towards normal LO2 cells. At concentrations of 2 to 8 μM for 24 hours, it triggers cell cycle arrest at the G1 phase in MCF-7 cells and enhances apoptotic rates in both MCF-7 and MCF-7/ADR cells over 48 hours. Furthermore, this compound increases the expression of apoptosis-inducing proteins cleaved-caspase-3 and cleaved-PARP in MCF-7 cells and modifies the expression of anti-apoptotic and pro-apoptotic proteins in MCF-7/ADR cells within 24 hours of treatment. Notably, even at low doses (0.1 μM for 24 hours), it induces apoptosis by encouraging ROS accumulation in MCF-7/ADR cells. Additionally, it bolsters the intracellular accumulation of ADR and Rh123 in MCF-7/ADR cells and reduces P-gp expression, indicating a decrease in drug resistance mechanisms. Detailed cell proliferation assays revealed IC50 values indicating the compound's efficacy across several cancer cell types with minimal impact on normal cells, underscoring its potential as a selective cancer therapeutic agent [1].
In vivo	Intravenous administration of the Topoisomerase I inhibitor 5 at doses of 1 mg/kg and 10 mg/kg every two days for a period of 21 days resulted in a significant decrease in tumor growth in an animal model utilizing Balb/c nude mice, which were injected with 10^6 MCF-7 cells in the left flank for 7 days. Notably, the tumor inhibition ratio reached 32.4% at a dosage of 1 mg/kg and 7.2% at 10 mg/kg, highlighting the compound's efficacy in reducing tumor size.

Molecular Weight	372.46
Formula	C24H24N2O2
CAS No.	2513461-95-3

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Topoisomerase I inhibitor 5 2513461-95-3 inhibitor inhibit

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