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2055362-72-4

中文名稱 Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
英文名稱 Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
CAS 2055362-72-4
分子式 C22H15NO4S2
分子量 421.49
MOL 文件 2055362-72-4.mol
2055362-72-4 結構式 2055362-72-4 結構式

基本信息

中文別名
化合物 T13379
化合物(Z)-LEUKADHERIN-1
英文別名
ADH-503 free base
Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-

物理化學性質

沸點634.7±65.0 °C(Predicted)
密度1.50±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.11±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

常見問題列表

生物活性
(Z)-Leukadherin-1 (ADH-503 free base) 是一種具有口服活性的,變構的 CD11b 激動劑。(Z)-Leukadherin-1 可以導致與腫瘤相關的巨噬細胞重新極化,減少腫瘤浸潤性免疫抑制骨髓細胞的數(shù)量,并增強樹突狀細胞的反應。
靶點

CD11b

體外研究

(Z)-Leukadherin-1 (ADH-503 free base; 4 μM; 8 days) reduces the numbers of total tumor-infiltrating CD11b + cells and subsets of CD11b + monocytes, granulocytes, eosinophils, and macrophages.

體內研究

(Z)-Leukadherin-1 (ADH-503 free base; oral gavage; 30, 60, or 120 mg/kg; twice a day for 60 days) delayes tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival.
(Z)-Leukadherin-1 (oral gavage; 30, 100 mg/kg; twice a day; on days 1 and 5) has the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively.

Animal Model: KPC mice [p48-CRE/Lox-stop-Lox(LSL)-Kras G12D /p53 flox/flox ]
Dosage: 30, 60, or 120 mg/kg
Administration: Oral gavage; 60 days
Result: Delayed tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival.
Animal Model: Male rats
Dosage: 30, 100 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage twice a day; on days 1 and 5
Result: Had the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively.
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