MSA-2 dimer

MSA-2 dimer is a selective, orally active non-nucleotide STING agonist ( K d =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 In Vivo MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival . MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression . MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors . MSA-2 dimer (60 mg/kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues . 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 . MSA-2 dimer also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:Kd: 145 μM (STING)

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