STING Agonist 12L

一种STING激动剂；能够与野生型STING结合（IC50=1.15µM），以及STING的R232H、AQ和Q突变体（IC50值分别为1.06µM、0.61µM和1.12µM）。该激动剂在THP-1细胞和RAW 264.7细胞中诱导报告基因表达（EC50值分别为0.38µM和12.94µM）。在5µM时，该激动剂可诱导THP-1细胞中IFNB1、CXCL10和IL6 mRNA的表达。在B16/F10小鼠黑色素瘤模型中，以10mg/kg的剂量给药时，可增加血浆中IFN-β水平，减少肿瘤体积和肺转移的数量。A STING agonist; binds to wild-type STING (IC50 = 1.15 µM), as well as the STING R232H, AQ, and Q variants (IC50s = 1.06, 0.61, and 1.12 µM, respectively); induces reporter gene expression in THP-1 and RAW 264.7 cells (EC50s = 0.38 and 12.94 µM, respectively); induces IFNB1, CXCL10, and IL6 mRNA expression in THP-1 cells at 5 µM; increases plasma IFN-β levels and reduces tumor volume and the number of lung metastases in a B16/F10 murine melanoma model at 10 mg/kg.分子式C18H10FN5O3分子量363.3O=C(O)C1=CC(F)=C(C#C)C=C1NC(C2=NN=C(C3=CC=NN=C3)C=C2)=O