MSA-2 dimer 是一种具有选择性和口服活性的非核苷酸 STING 激动剂 (K_d=145 μM)，有长期抗肿瘤和免疫原活性。MSA-2 dimer 作为非共价二聚体与 STING 结合，其渗透率高于循环二核苷酸。

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.

Solid

Kd: 145 μM (STING)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098.

In Vitro: DMSO : 70 mg/mL (123.10 mM; Need ultrasonic)配制储备液