STING agonist-12

Modify Date: 2024-01-04 11:18:39

STING agonist-12 Structure
STING agonist-12 structure
Common Name STING agonist-12
CAS Number 2259624-71-8 Molecular Weight 490.88
Density N/A Boiling Point N/A
Molecular Formula C25H19ClF4N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of STING agonist-12


STING agonist-12 (Compound 53) is a potent, orally active human STING activator with an EC50 of 185 nM[1].

 Names

Name STING agonist-12

 STING agonist-12 Biological Activity

Description STING agonist-12 (Compound 53) is a potent, orally active human STING activator with an EC50 of 185 nM[1].
Related Catalog
Target

EC50: 185 nM (STING)[1]

In Vitro STING agonist-12 (Compound 53) (10 μM) shows excellent pan-polymorph activity across the panel of STING proteins (92%, 107% and 92% against R232, H232 and HAQ, respectively) in HEK293T cells[1]. STING agonist-12 is not active at mouse STING[1].
In Vivo STING agonist-12 (Compound 53) (5 mpk for i.v.; 10 mpk for p.o.) is well-absorbed with a short terminal half-life[1]. Animal Model: Balb/c mice (n=3)[1] Dosage: 5 or 10 mpk Administration: Lateral tail vein or oral gavage (Pharmacokinetic Analysis) Result: Pharmacokinetic profile of STING agonist-12 (Compound 53) in mouse[1]. Route DOSE (mpk) AUC (ng/mL*h) T1/2 (h) Cmax (ng/mL) Vd (mL/kg) F (%) IV 5 1215 1.41 1867 2689 NA PO 10 2090 NA 1723 NA 86
References

[1]. Pryde DC, et al. The discovery of potent small molecule activators of human STING. Eur J Med Chem. 2021 Jan 1;209:112869.

 Chemical & Physical Properties

Molecular Formula C25H19ClF4N2O2
Molecular Weight 490.88