| Description |
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1].
|
| Related Catalog |
|
| Target |
Kd: 145 μM (STING)[1]
|
| In Vivo |
MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1]. MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors[1]. MSA-2 dimer (60 mg/kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues [1]. MSA-2 dimer (THP-1 cells) induces phosphorylation of both TBK1 and IR. MSA-2 dimer (10 μM and 33 μM; macrophages) induces IFN-β[1]. MSA-2 dimer also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes[1]. Animal Model: B16F10 tumor-bearing mice Dosage: 60 mg/kg Administration: P.o.; 50 days Result: Inhibited tumor growth and prolonged overall survival. Animal Model: C57BL6 mice Dosage: 40 mg/kg Administration: S.c.; 25 days Result: Induced complete tumor regression. Animal Model: C57BL6 mice Dosage: 60 mg/kg Administration: P.o.; 4 hours Result: Increased proinflammatory cytokine (IFN-β) level in tumors. Animal Model: C57BL6 mice Dosage: 50 mg/kg Administration: S.c.; 4 hours Result: MSA-2 concentrations were observed in tumors than in plasma or other nontumor tissues.
|
| References |
[1]. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098.
|
