| Description | (Z)-Leukadherin-1 (ADH-503 free base) is an allosteric agonist of CD11b. |
| In vitro | (Z)-Leukadherin-1 (4 μM) treatment reduces the numbers of total tumor-infiltrating CD11b+ cells and subsets of CD11b+ monocytes, eosinophils, granulocytes, and macrophages. (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[1]. |
| In vivo | (Z)-Leukadherin-1 shows a mean half-life of 4.68 and 3.95 h, a maximum concentration of 1716 and 2594 ng/ml and AUC(0-t) in the plasma of 6950 and 13962 ng·h/ml at 30 and 100 mg/kg dosing, respectively. In KPC mice, (Z)-Leukadherin-1 (30, 60, or 120 mg/kg; gavage) delayes tumor progression and leads to a significantly decreased tumor burden in time-point analysis and improved overall survival[1]. |
| Synonyms | ADH-503 free base |
| molecular weight | 421.49 |
| Molecular formula | C22H15NO4S2 |
| CAS | 2055362-72-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4 mg/mL (9.49 mM), Sonication and heating to 60℃ are recommended. |
| References | 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). |