Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Dabfilon effectively inhibited PGHS-2 (IC50 = 0.19 μM), but had a much smaller effect on PGHS-1 (IC50 = 20 μM).

Darbufelone is a non-competitive inhibitor of PGHS-2 (Ki = 10 ± 5μM). Darbufelone can quench the fluorescence of PGHS-2 at a concentration of Kd = 0.98 ± 0.03μM at 325 nm (λ (ex) = 280 nm). To test Darbufelone's putative antiproliferative effect, A549, H520 and H460 cell lines were used to establish three different NSCLC pathological subtypes (adenocarcinoma, squamous cell carcinoma and large cell lung cancer, respectively). The increased concentration of bufafenone (5 to 60 μM) was tested for 72 hours. As the drug concentration increased, the cell growth inhibitory effects of these three cell lines gradually increased. The IC50 of A549 and H520 are 20 ± 3.6 and 21 ± 1.8μM respectively, while the IC50 of H460 is much lower (15 ± 2.7μM).

Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Dabfilon has oral activity in animal models of inflammation and arthritis and does not cause ulcers. When the mice were treated with bufafenone at a dose of 80 mg / kg / day, the tumor volume decreased in a time-dependent manner. In contrast, the lower dose of bufafenone (20 or 40 mg / kg / day) did not show any significant inhibition of tumor weight. At necropsy, the tumor weight of the mice treated with bufafenone (80 mg / kg / day) was reduced by 30.2% compared to the control group.

139340-56-0

C19H28N2O5S2

428.57

CI-1004 mesylate

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years