ADH-503 ((Z)-Leukadherin-1 choline) 是一种具有口服活性的，变构的 CD11b 激动剂。ADH-503 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。
货号:ajcx29096
CAS:2055362-74-6
分子式:C27H28N2O5S2
分子量：524.65
溶解度:DMSO: 21.43 mg/mL (40.85 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

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[1].

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[1]. 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[1]. Animal Model: KPC mice [p48-CRE/Lox-stop-Lox(LSL)-KrasG12D/p53flox/flox][1]

[1]. Panni RZ, et al. Agonism of CD11b reprograms innate immunity to sensitize pancreatic cancer to immunotherapies. Sci Transl Med. 2019 Jul 3;11(499).