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Chemical Structure| 42835-25-6 Chemical Structure| 42835-25-6

Structure of Flumequine
CAS No.: 42835-25-6

Chemical Structure| 42835-25-6

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Flumequine is a topoisomerase II inhibitor with IC50 of 15 μM. It is a synthetic chemotherapeutic antibiotic.

Synonyms: R-802; (±)-Flumequine

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Product Details of Flumequine

CAS No. :42835-25-6
Formula : C14H12FNO3
M.W : 261.25
SMILES Code : CC1CCC2=C3N1C=C(C(O)=O)C(=O)C3=CC(F)=C2
Synonyms :
R-802; (±)-Flumequine
MDL No. :MFCD00079298
InChI Key :DPSPPJIUMHPXMA-UHFFFAOYSA-N
Pubchem ID :3374

Safety of Flumequine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Flumequine

DNA

Isoform Comparison

Biological Activity

Target
  • Topo II

    Topo II, IC50:15 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
B16F10 cells 0–50 μM 72 hours To investigate the effect of flumequine on melanogenesis. Results showed that flumequine significantly increased extracellular and intracellular melanin content in B16F10 cells and promoted the expression of MITF and tyrosinase. Biomolecules. 2019 Oct 11;9(10):596
human lymphocytes 25 μg/ml 5 days To evaluate the effect of Flumequine on [3H]thymidine incorporation in PHA-stimulated human lymphocytes. Results showed that Flumequine significantly increased [3H]thymidine incorporation at 25 μg/ml. Antimicrob Agents Chemother. 1987 May;31(5):768-73
Micrococcus luteus DNA gyrase 625 μg/ml 30 minutes Compare the ability of Flumequine and other quinolones to inhibit the supercoiling activity of DNA gyrase, results showed Flumequine completely inhibited supercoiling activity at 625 μg/ml Antimicrob Agents Chemother. 1986 Apr;29(4):598-601

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish larvae Zebrafish larvae model Direct addition to culture medium 0–20 μM 72 hours To evaluate the effect of flumequine on melanogenesis in vivo. Results showed that flumequine significantly increased melanin pigmentation in zebrafish larvae without any toxicity. Biomolecules. 2019 Oct 11;9(10):596
Male Wistar rats Pubertal male rats Oral 53, 200, 750 mg/kg Daily for six weeks To evaluate the toxicological effects of FLU on the endocrine and immune systems. Results showed that weight gain was poorer in the FLU 750 group, with notably higher relative weights of the brain, adrenal and thyroid glands, and testes. Haematological and lipid profile parameters, cardiac markers, and inorganic phosphate significantly increased in the FLU 750 group. Blood glucose, oestradiol and serum concentrations of immunoglobulins G (IgG) and E (IgE) significantly decreased after treatment. The levels of interleukins 10 (IL-10) and 6 (IL-6) fell significantly in the FLU 200 and FLU 750 groups. Cytochrome P450, family 1, subfamily A, polypeptide 1 (CYP1A1) and cyclooxygenase-2 (Cox-2) expression amplified after treatment. Serum levels of free triiodothyronine (fT3) and free thyroxine (fT4) reduced in the FLU 200 and FLU 750 groups without changes in total T3 or T4 level. All doses of FLU significantly depressed concentrations of thyroid-stimulating hormone (TSH) and testosterone. Histopathology of thyroid glands from rats treated with FLU 750 showed degeneration and depletion of thyroid follicular epithelial cells. J Vet Res. 2018 Mar 30;62(1):87-96

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02068664 - Completed - United States, New Jersey ... More >> Adler Aphasia Center Maywood, New Jersey, United States, 07607 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.83mL

0.77mL

0.38mL

19.14mL

3.83mL

1.91mL

38.28mL

7.66mL

3.83mL

References

 

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