Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
- CAS号:2055362-72-4
- 英文名:Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
- 中文名:Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
- CBNumber:CB85488502
- 分子式:C22H15NO4S2
- 分子量:421.49
- MOL File:2055362-72-4.mol
- 沸点 :634.7±65.0 °C(Predicted)
- 密度 :1.50±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :4.11±0.10(Predicted)
Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-性质、用途与生产工艺
- 生物活性 (Z)-Leukadherin-1 (ADH-503 free base) 是一种具有口服活性的,变构的 CD11b 激动剂。(Z)-Leukadherin-1 可以导致与肿瘤相关的巨噬细胞重新极化,减少肿瘤浸润性免疫抑制骨髓细胞的数量,并增强树突状细胞的反应。
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靶点
CD11b
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体外研究
(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.
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体内研究
(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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