(Z)-Leukadherin-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

(Z)-Leukadherin-1 是 CD11b 的变构激动剂。

(Z)-Leukadherin-1 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.(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.

(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.

(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.

ADH-503 free base

Immunology/Inflammation

Complement System

ALK| ALK G1202R| ALK L1196M

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2055362-72-4

421.49

C22H15NO4S2

>98% (HPLC)

In Vitro:?DMSO : 4.55 mg/mL (10.80 mM)

C(\C=1OC(=CC1)C2=CC=C(C(O)=O)C=C2)=C\3/C(=O)N(CC4=CC=CC=C4)C(=S)S3

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(-20℃)

With Ice Pack

≥ 2 years