STING agonist A4

Chemical Structure : STING agonist A4

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货号: PC-24586Not For Human Use, Lab Use Only.

STING agonist A4 is a potent, specific STING agonist, effectively activates STING in both human THP1 and mouse RAW 264.7 cells with EC50 values of 0.06 and 14.15 μM, respectively.

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生物&药学活性

STING agonist A4 is a potent, specific STING agonist, effectively activates STING in both human THP1 and mouse RAW 264.7 cells with EC50 values of 0.06 and 14.15 μM, respectively.
A4 demonstrates remarkable binding affinities to various hSTING variants and mSTING with IC50 values ranging from 0.77 to 2.64 μM
A4 more effectively stabilizes STING in its active conformation, compared to SR-717.
A4 binds to hSTING REF protein with substantially better affinity than SR-717 (Kd = 3.23 vs 526 nM) in ITC assays.
A4 effectively activated the STING signaling pathway, induces phosphorylation of STING downstream proteins as TBK1, IRF3, and p65 in THP1 cells, displays remarkable capabilities in inducing the mRNA expression of target genes IFNB1 and IL6 in a concentration-dependent manner in RT-qPCR analysis.
A4 (5 and 10 mg/kg, i.v.) significantly elevated plasma IFN-β levels in C57BL/6 mice, significantly inhibited tumor growth, with tumor growth inhibition (TGI) rates of 51.23 and 74.45%, respectively B16.F10 xenograft mouse model.

物理化学性质&存储条件

分子量	375.22
分子式	C17H8F2LiN5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Lithium 4-Ethynyl-5-fluoro-2-(6-(4-fluoro-1H-imidazol-1-yl)pyridazine-3-carboxamido)benzoate

参考文献

1. Hou H, et al. J Med Chem. 2025 May 9. doi: 10.1021/acs.jmedchem.4c01873.

STING agonist A4

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STING agonist A4

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