(5Z)-2-氨基-5-[(4-羟基-3,5-二叔丁基苯基)亚甲基]-1,3-噻唑-4-酮
中文名称 | (5Z)-2-氨基-5-[(4-羟基-3,5-二叔丁基苯基)亚甲基]-1,3-噻唑-4-酮 |
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中文同义词 | (5Z)-2-氨基-5-[(4-羟基-3,5-二叔丁基苯基)亚甲基]-1,3-噻唑-4-酮;达布非龙,;5-((Z)-4-羟基-3,5-二叔丁基苯基亚甲基)-2-亚氨基-4-噻唑烷酮;达布飞龙;达布非隆;化合物 T10960;达布非酮 |
英文名称 | (5Z)-2-Amino-5-[(4-hydroxy-3,5-ditert-butyl-phenyl)methylidene]-1,3-thiazol-4-one |
英文同义词 | (5z)-2-amino-5-[(4-hydroxy-3,5-ditert-butyl-phenyl)methylidene]-1,3-thiazol-4-one;5-((z)-3,5-di-tert-butyl-4-hydroxybenzylidene)-2-imino-4-thiazolidinone;(Z)-2-AMino-5-(3,5-di-tert-butyl-4-hydroxybenzylidene)thiazol-4(5H)-one;darbufelone;CS-490;(5Z)-2-amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one;4(5H)-Thiazolone, 2-amino-5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-, (5Z)-;(5Z)-2-Amino-5-[(4-hydroxy-3,5-ditert-butyl-phenyl)methylide... |
CAS号 | 139226-28-1 |
分子式 | C18H24N2O2S |
分子量 | 332.46 |
EINECS号 | 1312995-182-4 |
相关类别 | |
Mol文件 | 139226-28-1.mol |
结构式 | ![]() |
(5Z)-2-氨基-5-[(4-羟基-3,5-二叔丁基苯基)亚甲基]-1,3-噻唑-4-酮 性质
沸点 | 448.6±55.0 °C(Predicted) |
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密度 | 1.18±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | 溶于二甲基亚砜 |
形态 | 固体 |
酸度系数(pKa) | 9.98±0.50(Predicted) |
颜色 | 白色至米白色 |
IC50: 0.19 μM (PGHS-2), 20 μM (PGHS-1)
Darbufelone is a noncompetitive inhibitor of PGHS-2 (K i =10±5 μM). Darbufelone quenches the fluorescence of PGHS-2 at 325 nm (lambda(ex)=280 nm) with K d =0.98±0.03 μM.To test the putative anti-proliferative effect of Darbufelone, A549, H520 and H460 cell lines are used, which are established from three distinct pathological subtypes of NSCLC (adenocarcinoma, squamous and large cell lung cancer respectively). Increasing concentrations of Darbufelone, ranging from 5 to 60 μM, are tested for 72 h. The cell growth inhibition of these three cell lines gradually increases with higher drug concentration. The IC 50 of A549 and H520 are 20±3.6 and 21±1.8 μM, respectively, while the H460 has much lower IC 50 (15±2.7 μM).
Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. When mice are treated with Darbufelone at dosage of 80 mg/kg/day, the tumor volumes decrease in a time-dependent manner. 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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-101438 | (5Z)-2-氨基-5-[(4-羟基-3,5-二叔丁基苯基)亚甲基]-1,3-噻唑-4-酮 Darbufelone | 139226-28-1 | 1mg | 2000元 |