| Description | Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1. |
| In vitro | Darbufelone (5 - 60 μM) 在A549、H520和H460细胞系中增强了对细胞生长的抑制效果，其半抑制浓度（IC50）分别为20、21和15 μM[2]。 |
| In vivo | Darbufelone（80 mg/kg/日）能够随时间依赖性地减少肿瘤体积。Darbufelone（20或40 mg/kg/日）对肿瘤重量的抑制没有显著性。经解剖观察，Darbufelone（80 mg/kg/日）使肿瘤重量降低了30.2%[2]。 |
| Target activity | PGHS1:20 μM , PGHS2:0.19 μM |
| Synonyms | 达布非酮, CI-1004 |
| molecular weight | 332.46 |
| Molecular formula | C18H24N2O2S |
| CAS | 139226-28-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (135.35 mM) |
| References | 1. Johnson AR, et al. Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol. Biochemistry. 2001 Jun 26;40(25):7736-45. 2. Ye X, et al. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol. 2010 Jul;66(2):277-85. |