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ADH-503

Chemical Structure : ADH-503

CAS No.: 2055362-72-4

ADH-503 (ADH503, GB1275, Leukadherin-1 choline)

Catalog No.: PC-72987Not For Human Use, Lab Use Only.

ADH-503 (GB1275, Leukadherin-1 choline) is a small-molecule allosteric agonist of CD11b that can render tumors more sensitive to checkpoint blockade.

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Biological Activity

ADH-503 (GB1275, Leukadherin-1 choline) is a small-molecule allosteric agonist of CD11b that can render tumors more sensitive to checkpoint blockade.
ADH-503 rapidly decreased the genes involved in IL-1 signaling, increased the expression of cytokines involved in T cell and DC trafficking.
ADH-503 reduced the regulatory T cell (Treg) recruitment of cytokines CCL17 and CCL22 in PDAC-activated macrophages, down-regulated TGF-β1, IL-1α, and IL-1β and reduced alternative activation markers arginase-1 (Arg1), YM1, and Retnlα while upregulating type I interferons (IFNα1 and IFNβ) and T cell recruitment factors (CXCL9, CXCL10, and CXCL11).
ADH-503 reduced the numbers of total tumor-infiltrating CD11b+cells and subsets of CD11b+ monocytes, granulocytes, eosinophils, and macrophages on myeloid cells, improves T cell responses in vivo, induces the accumulation of CD103+ cDCs in the tumor.
ADH-503 impairs tumor growth and improves survival in orthotopic models and KPC GEMMs, also improves the efficacy of chemotherapy.

Physicochemical Properties

M.Wt 524.65
Formula C27H28N2O5S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-hydroxy-N,N,N-trimethylethan-1-aminium (Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoate

References

1. Panni RZ, et al. Sci Transl Med. 2019 Jul 3;11(499). pii: eaau9240. doi: 10.1126/scitranslmed.aau9240.
2. Geraghty T, et al. Front Oncol. 2020 May 21;10:748.

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