(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 In Vitro (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: KPC mice [p48-CRE/Lox-stop-Lox(LSL)-Kras G12D /p53 flox/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. IC50& Target:CD11b
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(Z)-Leukadherin-1
CAS number:2055362-72-4(DMSO) molecular formula:C22H15NO4S2
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| Chinese alias | (Z)-白细胞粘附素-1 | ||
| English alias | - | ||
| CAS number | 2055362-72-4(DMSO) | molecular formula | C22H15NO4S2 |
| molecular weight | 421.49 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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