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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[1]. | [in vivo]
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].
| Parameter | Compound 4a | | T1/2 (h) | 10.54 ± 4.10 | | Vss (L/kg) | >17.74 ± 5.29 | | CL (L/h/kg) | 2.12 ± 0.27 | | AUClast (μg h/mL) | 4.20 ± 0.26 | | AUC∞ (μg h/mL) | >4.78 ± 0.59 | |
| Animal Model: | Female BALB/c mice aged 6 weeks[1] | | Dosage: | 0.015 mg/kg, 1.5 mg/kg | | Administration: | Intravenous injection; every other day; a week | | Result: | Inhibited tumor growth in both doses and caused 57% inhibition at a concentration of 1.5 mg/kg on the 17th day without weight loss. |
| [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. DOI:10.1021/acs.jmedchem.1c01795 |
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