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139340-56-0

中文名稱 甲磺酸達(dá)布非龍
英文名稱 Darbufelone mesilate
CAS 139340-56-0
分子式 C18H24N2O2S.CH4O3S
分子量 428.57
MOL 文件 139340-56-0.mol
139340-56-0 結(jié)構(gòu)式 139340-56-0 結(jié)構(gòu)式

基本信息

中文別名
甲磺酸達(dá)布非隆
甲磺酸達(dá)布非龍
(5Z)-2-氨基-5-[(3,5-二叔丁基-4-羥基苯基)亞甲基]-1,3-噻唑-4-酮甲磺酸鹽
英文別名
CI 1004
CI-1004 mesylate
DARBUFELONE MESILATE
Darbufelone (mesylate)
(5Z)-2-Amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one methanesulfonate

物理化學(xué)性質(zhì)

儲存條件4°C, protect from light
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to light yellow

常見問題列表

生物活性
Darbufelone mesylate (CI-1004 mesylate) 雙重抑制細(xì)胞 PGF2α 和 LTB4 產(chǎn)生。Darbufelone 有效抑制 PGHS-2 (IC50=0.19 μM),但對 PGHS-1 效力要低得多 (IC50=20 μM)。
靶點

PGF

LTB 4

PGHS-2

0.19 μM (IC 50 )

PGHS-1

20 μM (IC 50 )

體外研究

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) .

體內(nèi)研究

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.

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