STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization.
STING agonist-17 (compound 4a) inhibits the activity of four major CYP isozymes (CYP1A2, CYP2C9, CYP2C19 and CYP2D6) with IC50 values > 100 μM and for CYP3A4 with an IC50 = 4.2 μM[1].STING agonist-17 (compound 4a) (0-2 μM, 24 hours) induces IFN-β secretion with the EC50 of 2.0 nM[1].STING agonist-17 (compound 4a) (2 nM, 10 nM, 6 hours) can induce the expression of signal transduction factors[1].The pharmacokinetic parameters of Compound 4a in vitro[1].
STING agonist-17 (compound 4a) (Intravenous injection; 0.015 mg/kg, 1.5 mg/kg; every other day; a week) has an inhibitory effect on tumor growth in CT26 cells-derived colon carcinoma female BALB/c mice[1].The pharmacokinetic parameters of Compound 4a in vivo[1].
References:
[1]. Min Jae Jeon, et al. Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor. J Med Chem. 2022 Apr 14;65(7):5407-5432.