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编 号:F621076
分子式:C22H15NO4S2
分子量:421.49
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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生物活性:
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.

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)-KrasG12D/p53flox/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.

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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