ChemicalBook CAS DataBase List 2377881-92-8

2377881-92-8

Name	Benzo[b]thiophene-2-butanoic acid, 5,5'-(1,3-propanediyl)bis[6-methoxy-γ-oxo-
CAS	2377881-92-8
Molecular Formula	C29H28O8S2
Molecular Weight	568.66
MOL File	2377881-92-8.mol

Chemical Properties

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

Uses

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].
? 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^[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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