STING agonist-12

• CAT Number: I043439
• CAS Number: 2259624-71-8
• Molecular Formula: C25H19ClF4N2O2
• Molecular Weight: 490.88
• Purity: ≥95%
• Synonyms: 1-[(2-chloro-6-fluorophenyl)methyl]-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]indole-6-carboxamide
• InChI: InChI=1S/C25H19ClF4N2O2/c1-25(2)17-7-6-13(23(33)31-11-15-20(29)9-14(27)10-21(15)30)8-22(17)32(24(25)34)12-16-18(26)4-3-5-19(16)28/h3-10H,11-12H2,1-2H3,(H,31,33)
• InChIKey: OEBVYNULNKSONR-UHFFFAOYSA-N
• SMILES: CC1(C2=C(C=C(C=C2)C(=O)NCC3=C(C=C(C=C3F)F)F)N(C1=O)CC4=C(C=CC=C4Cl)F)C

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

Reference

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