甲磺酸达布非龙

甲磺酸达布非龙

中文名称甲磺酸达布非龙
中文同义词(5Z)-2-氨基-5-[(3,5-二叔丁基-4-羟基苯基)亚甲基]-1,3-噻唑-4-酮甲磺酸盐;甲磺酸达布非龙;甲磺酸达布非隆;化合物 T10960L
英文名称Darbufelone mesilate
英文同义词CI 1004;DARBUFELONE MESILATE;(5Z)-2-Amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one methanesulfonate;Darbufelone (mesylate);CI-1004 mesylate;Darbufelone mesylate (CI-1004 mesylate)
CAS号139340-56-0
分子式C19H28N2O5S2
分子量428.56
EINECS号
相关类别
Mol文件139340-56-0.mol
结构式甲磺酸达布非龙 结构式

甲磺酸达布非龙 性质

储存条件4°C, protect from light
溶解度溶于二甲基亚砜
形态固体
颜色白色至浅黄色

甲磺酸达布非龙 用途与合成方法

Darbufelone mesylate (CI-1004 mesylate) 双重抑制细胞 PGF2α 和 LTB4 产生。Darbufelone 有效抑制 PGHS-2 (IC50=0.19 μM),但对 PGHS-1 效力要低得多 (IC50=20 μM)。

PGF

LTB 4

PGHS-2

0.19 μM (IC 50 )

PGHS-1

20 μM (IC 50 )

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

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-101438A甲磺酸达布非龙
Darbufelone mesylate
139340-56-05mg1500元
2024/04/30HY-101438A甲磺酸达布非龙
Darbufelone mesylate
139340-56-025mg5500元

甲磺酸达布非龙 上下游产品信息

"甲磺酸达布非龙"相关产品信息
甲磺酸左氧氟沙星 甲磺酸培氟沙星 伊马替尼 过氧化乙酸叔丁酯 甲磺酸酚妥拉明 三氟甲磺酸 丙烯酸正丁酯 二乙二醇丁醚 噻嗪酮 甲磺酸加替沙星 乙酸丁酯 (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 甲磺酸帕珠沙星 乙二醇单丁醚 氰氟草酯 油酸丁酯 甲基磺酸 甲磺酸达布非龙
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