Home DNA Damage/DNA Repair Topoisomerase inhibitor Flumequine

research use only

Flumequine Topoisomerase inhibitor

Flumequine (R-802) is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.

Flumequine Topoisomerase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 261.25

Purity & Quality Control

Batch: S318101 DMSO]3 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.62%
99.62

Related Products

Signaling Pathway

Topoisomerase Signaling Pathways

Topoisomerase Signaling Pathway

Mechanism of Action

Targets
Topo II [1]
15 μM

In vitro
In vitro

Flumequine inhibits eukaryotic topoisomerase II, which is responsible for the double-strand DNA breakage reaction as well as bacterial gyrase, inhibitory effects of this compound on topoisomerase II are high relative to the influence on bacterial gyrase. [1] It has minimum inhibitory concentration (MIC) ranging from 0.06 μg/mL to 32 μg/mL in 12 clinical A. salmonicida isolates. This chemical enhibits high E(max) values of 16 for the most resistant isolates, which indicates an important contribution of efflux to the resistance phenotype. Its accumulation experiments confirmes that high E(max) values are associated with a much lower level of accumulation. [2]

In Vivo
In vivo

Flumequine (4000 ppm, oral diet) induces dose-dependent DNA damage in the stomach, colon, and urinary bladder of adult mice at 3 hours but not at 24 hours after its administration. [1] This compound shows the bioavailability of 44.7% following oral administration of medicated feed in Atlantic salmon. It results in the volumes of distribution at steady state of 3.5 L/kg, elimination half-life (t 1/2) of 22.8 hours and area under plasma drug concentration-time curve (AUC) of 140 μg×hours/mL following intravenous administration in Atlantic salmon. [3] This chemical (100 mg/L) reduces the mean length of root, hypocotyle, cotyledon and the mean number of secondary roots in aquatic weed Lythrum salicaria L. [4] The compound (10 mg/kg, oral) results in the volumes of distribution at steady-state (Vss) of 2.41 L/kg (cod) and 2.15 L/kg (wrasse) following intravenous administration. Total body clearances (Cl) are 0.024 L/h.kg (cod) and 0.14 L/h.kg (wrasse) and the elimination half-lives (t1/2 λ z) are calculated to be 75 hours (cod) and 31 hours (wrasse) after this compound (10 mg/kg, oral) administration. The oral bioavailabilities (F) are calculated to be 65% (cod) and 41% (wrasse) following oral administration of this chemical. [5]

References
  • https://pubmed.ncbi.nlm.nih.gov/12377980/
  • https://pubmed.ncbi.nlm.nih.gov/15314197/
  • https://pubmed.ncbi.nlm.nih.gov/7625789/
  • https://pubmed.ncbi.nlm.nih.gov/10705552/
  • https://pubmed.ncbi.nlm.nih.gov/11110104/

Chemical Information

Molecular Weight 261.25 Formula

C14H12FNO3
CAS No. 42835-25-6 SDF Download SDF
Synonyms R-802
Smiles CC1CCC2=C3N1C=C(C(=O)C3=CC(=C2)F)C(=O)O

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 3 mg/mL ( (11.48 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.