1H-Indole-6-carboxamide, 1-[(2-chloro-6-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]-
- CAS No.
- 2259624-71-8
- Chemical Name:
- 1H-Indole-6-carboxamide, 1-[(2-chloro-6-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]-
- Synonyms
- C53;STING agonist C53;STING activator Compound 53;STING activator Compound 53, 10 mM in DMSO;1-(2-chloro-6-fluorobenzyl)-3,3-dimethyl-2-oxo-N-(2,4,6-trifluorobenzyl)indoline-6-carboxamide;1-[(2-chloro-6-fluoro-phenyl)methyl]-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]indoline-6-carboxamide;1-[(2-chloro-6-fluorophenyl)methyl]-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]-2,3-dihydro-1H-indole-6-carboxamide;1H-Indole-6-carboxamide, 1-[(2-chloro-6-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]-;Inhibitor,HEK293T,STING agonist-12,MPYS,STING agonist12,STING,STING agonist 12,STING activator Compound 53,TMEM173,inhibit,ERIS,Stimulator of Interferon Genes,MITA
- CBNumber:
- CB010785689
- Molecular Formula:
- C25H19ClF4N2O2
- Molecular Weight:
- 490.88
- MDL Number:
- MOL File:
- 2259624-71-8.mol
1H-Indole-6-carboxamide, 1-[(2-chloro-6-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]- Properties
Boiling point | 628.4±55.0 °C(Predicted) |
---|---|
Density | 1.392±0.06 g/cm3(Predicted) |
storage temp. | 4°C, protect from light |
solubility | DMSO : 250 mg/mL (509.29 mM; Need ultrasonic) |
form | A crystalline solid |
pka | 13.31±0.40(Predicted) |
color | Light yellow to yellow |
1H-Indole-6-carboxamide, 1-[(2-chloro-6-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]- Chemical Properties,Uses,Production
Uses
STING agonist-12 (Compound 53) is a potent, orally active human STING activator with an EC50 of 185 nM[1].
Biological Activity
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].
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].
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storage
Store at -20°C
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.
1H-Indole-6-carboxamide, 1-[(2-chloro-6-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
1H-Indole-6-carboxamide, 1-[(2-chloro-6-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]- Suppliers
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