Home DNA Damage/DNA Repair Topoisomerase inhibitor Flumequine For research use only.

Flumequine

Synonyms: R-802

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

Flumequine Chemical Structure

Flumequine Chemical Structure

CAS No. 42835-25-6

Purity & Quality Control

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

Flumequine Related Products

Signaling Pathway

Topoisomerase Signaling Pathways

Topoisomerase Signaling Pathway

Biological Activity

Description Flumequine(R-802) is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
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 FL on topoisomerase II are high relative to the influence on bacterial gyrase. [1] Flumequine has minimum inhibitory concentration (MIC) ranging from 0.06 μg/mL to 32 μg/mL in 12 clinical A. salmonicida isolates. Flumequine enhibits high E(max) values of 16 for the most resistant isolates, which indicates an important contribution of efflux to the resistance phenotype. Flumequine 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] Flumequine shows the bioavailability of 44.7% following oral administration of medicated feed in Atlantic salmon. Flumequine 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] Flumequine (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] Flumequine (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 Flumequine (10 mg/kg, oral) administration. The oral bioavailabilities (F) are calculated to be 65% (cod) and 41% (wrasse) following oral administration of Flumequine. [5]

Chemical Information & Solubility

Molecular Weight 261.25 Formula

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


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In vivo
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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

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