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Cat. No. M9776
Darbufelone Structure

CI-1004; PD-136095-0073

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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Darbufelone (CI-1004) is a dual inhibitor of cellular PGF2α and LTB4 production, it is also a COX-2 inhibitor potentially for the treatment of rheumatoid arthritis. Darbufelone potently inhibits PGHS-2 (IC50=0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM). The IC50 of A549 and H520 are 20±3.6 and 21±1.8 μM, respectively, while the H460 has much lower IC50 (15±2.7 μM). 

Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. The tumor volumes decrease in a time-dependent manner on mice treated with Darbufelone (80 mg/kg/day). In contrast, lower dose of Darbufelone (20 or 40 mg/kg/day) dos not show any significant inhibition of tumor weight. At necropsy, the tumor weight in mice treated with Darbufelone (80 mg/kg/day) is reduced by 30.2% in comparison with control group.

Cell Experiment
Cell lines A549, NCI-H520 and NCI-H460 cells
Preparation method In brief, tumor cells growing in log-phase are trypsinized and seeded at 5×103 cells per well into 96-well plates and allowed to attach overnight. Medium in each well is replaced with fresh medium or medium containing various concentrations of Darbufelone (5-60 μM) in at least triplicate wells. Cells are cultured to another 72 h. After treatment, 1/10 volume of MTT solution (5 mg/mL) is added to each well, and the plate is incubated at 37°C for another 4 h. Two hundred microliters of DMSO is added to each well to solubilize the MTT-formazan product after removal of the medium. Absorbance at 595 nm is measured with a multi-well spectrophotometer. Growth inhibition is calculated as a percentage of the untreated controls.
Concentrations 5-60 μM
Incubation time 72 h
Animal Experiment
Animal models C57Bl/6 male mice implanted Lewis Lung Carcinoma cells
Formulation CMC-Na
Dosages 20, 40, and 80 mg/kg/day
Administration gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 332.46
Formula C18H24N2O2S
CAS Number 139226-28-1
Purity >98%
Storage -20°C, dry, sealed

Dual inhibition of COX-2/5-LOX blocks colon cancer proliferation, migration and invasion in vitro
Xiao-Hang Che, et al. Oncol Rep. 2016 Mar;35(3):1680-8. PMID: 26707712.

Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo
Xiaolei Ye, et al. Cancer Chemother Pharmacol. 2010 Jul;66(2):277-85. PMID: 20352217.

Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol
A R Johnson, et al. Biochemistry. 2001 Jun 26;40(25):7736-45. PMID: 11412128.

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Keywords: Darbufelone, CI-1004; PD-136095-0073 supplier, Prostaglandin Receptor, inhibitors

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