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Topo I/COX-2-IN-1

Catalog No. T61939

Topo I/COX-2-IN-1 (1H-30) is a potent Topo I/COX-2 inhibitor with the IC50 of 0.24 μM and 4.42 μM for COX-2 and Topo I, respectively. Topo I/COX-2-IN-1 induces apoptosis and inhibits migration of cancer cells, shows anti-cancer activity.

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

Topo I/COX-2-IN-1, 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

Chemical Properties

Storage & Solubility Information

Description	Topo I/COX-2-IN-1 (1H-30) is a potent Topo I/COX-2 inhibitor with the IC50 of 0.24 μM and 4.42 μM for COX-2 and Topo I, respectively. Topo I/COX-2-IN-1 induces apoptosis and inhibits migration of cancer cells, shows anti-cancer activity.
In vitro	Topo I/COX-2-IN-1 (1H-30) exhibits potent anti-tumor properties, effectively halting tumor cell proliferation and triggering apoptosis through dose-responsive enhancement of caspase-3 activity over a 24-hour exposure (0-100 μM). Moreover, at concentrations ranging from 0.04 to 0.37 μM over 48 hours, it significantly curtails cell migration, particularly at 0.37 μM, while concurrently depressing MMP-9 expression in HGC-27 and RKO cells. Furthermore, at a 10 μM concentration and 48-hour exposure, it obstructs the activation of the NF-κB signaling pathway in cancer cells. In various colon cancer cell lines (HGC-27, RKO, HT-29, SGC-7901, and CT26.WT), it demonstrated a remarkable capability to inhibit cell proliferation, presenting IC50 values that underscore its efficacy. Additionally, apoptosis analysis revealed a marked increase in caspase-3 positive cells, particularly at a 10 μM concentration, indicating its apoptotic potency. Also, it significantly induced cell cycle arrest in the G2/M phase, highlighting its diverse mechanisms of action against cancer cell growth and spread.
In vivo	Topo I/COX-2-IN-1 (1H-30), administered through intraperitoneal injection at a dosage of 100 mg/kg twice daily for 14 days, may suppress tumor growth in BALB/c mice infected with CT26.WT colon cancer cells by enhancing caspase-3 expression while reducing MMP-9 and COX-2 levels, thereby promoting apoptosis. In studies involving BALB/c mice, this regimen led to a notable decrease in tumor size and weight without adversely affecting body weight or organ health. Additionally, when tested in SD rats with the same dosage but administered once, Topo I/COX-2-IN-1 (1H-30) displayed pharmacokinetic parameters including a half-life (t 1/2) of 1.56 hours, time to reach maximum concentration (T max) of 0.67 hours, maximum serum concentration (C max) of 20.19 μg/mL, area under the curve from zero to last measurable concentration (AUC 0-t) of 18.20 mg/L h, and area under the curve from zero to infinity based on observed data (AUC 0 inf_obs) of 18.60 mg/L h.

Molecular Weight	400.83
Formula	C21H18ClFN2O3

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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Tech Support

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

Topo I/COX-2-IN-1 inhibitor inhibit

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