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Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
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- CAS号:
- 2055362-72-4
- 英文名:
- Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
- 英文别名:
- ADH-503 free base;Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-;ADH503,orally,macrophages,repolarization,dendritic,ADH 503,Complement System,allosteric,ADH-503,CD11b,tumorassociated,(Z)Leukadherin1,Inhibitor,(Z) Leukadherin 1,tumor-infiltrating,inhibit,immunosuppressive
- 中文名:
- Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
- 中文别名:
- 化合物 T13379;化合物(Z)-LEUKADHERIN-1
- CBNumber:
- CB85488502
- 分子式:
- C22H15NO4S2
- 分子量:
- 421.49
- MOL File:
- 2055362-72-4.mol
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Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-化学性质
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沸点:
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634.7±65.0 °C(Predicted)
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密度:
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1.50±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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4.11±0.10(Predicted)
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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
(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。
(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.
(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.
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Animal Model:
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KPC mice [p48-CRE/Lox-stop-Lox(LSL)-Kras
G12D
/p53
flox/flox
]
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Dosage:
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30, 60, or 120 mg/kg
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Administration:
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Oral gavage; 60 days
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Result:
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Delayed tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival.
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Animal Model:
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Male rats
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Dosage:
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30, 100 mg/kg (Pharmacokinetic Analysis)
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Administration:
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Oral gavage twice a day; on days 1 and 5
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Result:
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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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Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
上下游产品信息
上游原料
下游产品
Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-
生产厂家
2055362-72-4, Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]- 相关搜索:
- 化合物(Z)-LEUKADHERIN-1
- 化合物 T13379
- 2055362-72-4
- ADH503,orally,macrophages,repolarization,dendritic,ADH 503,Complement System,allosteric,ADH-503,CD11b,tumorassociated,(Z)Leukadherin1,Inhibitor,(Z) Leukadherin 1,tumor-infiltrating,inhibit,immunosuppressive
- ADH-503 free base
- Benzoic acid, 4-[5-[(Z)-[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-