ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
IC50&Target
CD11b
体外研究
ADH-503 ((Z)-Leukadherin-1 choline; 4 μM; 8 days) reduces the numbers of total tumor-infiltrating CD11b cells and subsets of CD11b monocytes, granulocytes, eosinophils, and macrophages.
体内研究
ADH-503 ((Z)-Leukadherin-1 choline; 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.
ADH-503 (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/p53]
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.
分子式
C27H28N2O5S2
分子量
524.65
CAS号
2055362-74-6
运输条件
Room temperature in continental US; may vary elsewhere.