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Description: Flumequine (formerly R-802; R 802; R802) is a synthetic quinolone, 1st generation and broad-spectrum chemotherapeutic antibiotic that was once used to treat bacterial infections but has been removed from market. It acts by inhibiting topoisomerase II with an IC50 of 15 μM. 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. Flumequine has minimum inhibitory concentration (MIC) ranging from 0.06 μg/mL to 32 μg/mL in 12 clinical A. salmonicida isolates.
References: Toxicol Sci. 2002 Oct;69(2):317-21; Antimicrob Agents Chemother. 1995 May;39(5):1059-64.
Chemical Name: 7-Fluoro-12-methyl-4-oxo-1-azatricyclo[7.3.1.05,13]trideca-2,5,7,9(13)-tetraene-3-carboxylic acid
InChi Key: DPSPPJIUMHPXMA-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H12FNO3/c1-7-2-3-8-4-9(15)5-10-12(8)16(7)6-11(13(10)17)14(18)19/h4-7H,2-3H2,1H3,(H,18,19)
SMILES Code: O=C(C(C1=O)=CN2C(C)CCC3=C2C1=CC(F)=C3)O
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: 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. 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.
Cell Assay: The Chinese hamster lung cell line CHL/IU is routinely maintained in monolayer culture in Dulbecco's modified MEM medium supplemented with 10% fetal bovine serum at 37°C under a 5% CO2 atmosphere. Exponentially growing cells are treated with Flumequine (R-802) dissolved in DMSO for 1 h. The dose range is chosen in order to obtain both damaged and highly damaged cells. Following Flumequine (R-802) treatment, cells are embedded in GP42 agarose dissolved in saline at 1%. Cell number and cell viability are determined for each dose.
Toxicol Sci. 2002 Oct;69(2):317-21; Antimicrob Agents Chemother. 1995 May;39(5):1059-64.
Purity ≥98%
COA
MSDS