A STING agonist
货号:ajcx22022
CAS:2412902-55-5
分子式:C30H37N7O6
分子量：591.7
溶解度:DMF: 10mg/mL,DMF:PBS (pH 7.2) (1:2): 0.3mg/mL,DMSO: 5mg/mL,Ethanol: 0.3mg/mL
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CAY10748 is an agonist of stimulator of interferon genes (STING; IC₅₀= 0.3794 µM in a competition binding assay).¹It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC₅₀s = 0.287 and >100 µM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β and the levels of chemokine (C-X-C motif) ligand 10 (CXCL10), and IL-6 in peripheral blood mononuclear cells (PBMCs) when used at a concentration of 10 µM. It also reduces tumor growth in a CT26 murine colon cancer model when administered at a dose of 0.15, but not 1.5, mg/kg.

1.Xi, Q., Wang, M., Jia, W., et al.Design, synthesis, and biological evaluation of amidobenzimidazole derivatives as stimulator of interferon genes (STING) receptor agonistsJ. Med. Chem.63(1)260-282(2019)