(Z)-Leukadherin-1

Modify Date: 2024-01-10 21:39:02

(Z)-Leukadherin-1 Structure
(Z)-Leukadherin-1 structure
Common Name (Z)-Leukadherin-1
CAS Number 2055362-72-4 Molecular Weight 421.49
Density N/A Boiling Point N/A
Molecular Formula C22H15NO4S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of (Z)-Leukadherin-1


(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumorassociated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses[1].

 Names

Name (Z)-Leukadherin-1

 (Z)-Leukadherin-1 Biological Activity

Description (Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumorassociated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses[1].
Related Catalog
Target

CD11b[1]

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

 Chemical & Physical Properties

Molecular Formula C22H15NO4S2
Molecular Weight 421.49
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