| Identification | Back Directory | [Name]
Benzo[b]thiophene-2-butanoic acid, 5,5'-(1,3-propanediyl)bis[6-methoxy-γ-oxo- | [CAS]
2377881-92-8 | [Synonyms]
MSA-2 dimer
Benzo[b]thiophene-2-butanoic acid, 5,5'-(1,3-propanediyl)bis[6-methoxy-γ-oxo- | [Molecular Formula]
C29H28O8S2 | [MOL File]
2377881-92-8.mol | [Molecular Weight]
568.66 |
| Chemical Properties | Back Directory | [Boiling point ]
817.6±65.0 °C(Predicted) | [density ]
1.376±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
4.10±0.17(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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].
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]. | [in vivo]
MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1].
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MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1].
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MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors[1].
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MSA-2 dimer (60 mg/kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues [1].
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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].
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MSA-2 dimer also exhibits dose-dependent antitumor activity[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. |
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Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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