Antibodies
Flumequine
- 貨號 Cat. No.
- S3181
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Flumequine
Catalog No.S3181
Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM. | |||||
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| Targets | Topoisomerase II | |||||
| IC50 | 15 μM [1] | |||||
| 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 | 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] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Topoisomerase II inhibitory assay | For the decatenation assay of topoisomerase II, 20 μL of reaction mixture containing 0.4 μg of kinetoplast DNA (kDNA) with 1 U of topoisomerase II and serial dilutions of Flumequine are incubated for 5 min at 37°C in buffer containing 20 mM Tris–HCl (pH 7.5), 120 mM KCl, 10 mM MgCl2, 1 mM ATP, 0.5 mM dithiothreitol, and 30 μg/mL of bovine serum albumin. After stopping the reaction by adding sarcosyl with gel-loading buffer, catenated and decatenated kDNAs are separated by agarose gel electrophoresis. The gels are stained with ethidium bromide and photographed using UV light (302 nm) with a Gel Print 200i/VGA, and the brightness of bands is traced with an Image Analyzer. Each band is quantified and the amount of DNA treated with each concentration of quinolone is measured to determine the 50% inhibitory concentration against DNA gyrase and topoisomerase II. |
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References
Chemical Information
| Molecular Weight (MW) | 261.25 |
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| Formula | C14H12FNO3 |
| CAS No. | 42835-25-6 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 3 mg/mL (11 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 1H,5H-Benzo[ij]quinolizine-2-carboxylic acid, 9-fluoro-6,7-dihydro-5-methyl-1-oxo- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.26125 | 2.6125 | - | - |
