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Topoisomerase I/II inhibitor 3

Catalog No. T61990

Topoisomerase I/II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) . By inhibiting PI3K /Akt/mTOR signaling pathway, Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis . Topoisomerase I/II inhibitor 3 has research value in liver cancer.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Topoisomerase I/II inhibitor 3 Chemical Structure

Topoisomerase I/II inhibitor 3, CAS N/A

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 1,520.00
50 mg	10-14 weeks	$ 1,980.00
100 mg	10-14 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	Topoisomerase I/II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) . By inhibiting PI3K /Akt/mTOR signaling pathway, Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis . Topoisomerase I/II inhibitor 3 has research value in liver cancer.
In vitro	Topoisomerase I/II inhibitor 3 (compound 7) (0-100 µM) disrupts DNA topology by intercalation, causing DNA damage [1]. At concentrations of 0-4 µM over 24 hours, it dose-dependently suppresses the proliferation, migration, and invasion of hepatocellular carcinoma (HCC) cells, including LM9 and HuH7 cells, through the inhibition of MMP-9 expression [1]. When administered at 0-14 µM for 48 hours, it significantly triggers apoptosis in LM9 and HuH7 cells, alongside dose-dependent mitochondrial dysfunction and reactive oxygen species (ROS) production [1]. Moreover, within the same timeframe at 0-7 µM, it diminishes Bcl-2 levels while enhancing the expression of pro-apoptotic proteins like Bax, cytochrome C, cleaved-caspase-3, and cleaved-caspase-9. This simultaneously obstructs the PI3K/Akt/mTOR pathway [1]. Assays conducted on HCC cell lines (HuH7 and LM9) with concentrations ranging from 0, 0.5, 1, 2, to 4 µM for 24 hours showed a hinderance in cell proliferation and colony formation in a concentration-dependent manner, with IC 50 values at 2.10 µM for LM9 and 1.93 µM for HuH7. Apoptosis analyses at 0, 1.8, 3.5, 7, and 14 µM over 48 hours confirmed enhanced apoptosis rates in a concentration-dependent manner. Western Blot analyses corroborated the reduction in Bcl-2 expression and an increase in apoptosis-related proteins, while also confirming the inhibition of the PI3K/Akt/mTOR signaling pathway [1].
In vivo	Topoisomerase I/II inhibitor 3, administered intraperitoneally (IP) at doses of 200, 250, and 400 mg/kg to male Kunming mice, resulted in mortality exclusively in the 400 mg/kg cohort, establishing the lethal dose (LD 50) between 250 and 400 mg/kg. The compound, dissolved in 5% DMSO and castor oil, was administered once to four groups of male Kunming mice, each group comprising 8 mice with body weights ranging from 19-22 mg. Observations over a two-week period showed no lethal effects in the 200 mg/kg and 250 mg/kg groups.

Molecular Weight	404.46
Formula	C24H24N2O4

Storage

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

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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/II inhibitor 3 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.