MSA-2 是可口服的非核苷酸STING激动剂，以具有纳摩尔亲和力的非共价二聚体形式与 STING 结合。它在同基因小鼠肿瘤模型中显示抗肿瘤活性，与抗 PD-1 协同作用，可刺激肿瘤分泌干扰素-β，诱导肿瘤消退，具有持久的抗肿瘤免疫。

MSA-2 is a potent and orally available non-nucleotide STING agonist.

MSA-2 is an agonist of stimulator of interferon genes (STING) has EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. In syngeneic mouse tumor models, subcutaneous and oral MSA-2 regimens were well tolerated and stimulated interferon-β secretion in tumors, induced tumor regression with durable antitumor immunity, and synergized with anti-PD-1 therapy.?Experimental and theoretical analyses showed that MSA-2 exists as interconverting monomers and dimers in solution, but only dimers bind and activate STING.?This model was validated by using synthetic covalent MSA-2 dimers, which were potent agonists.?Cellular potency of MSA-2 increased upon extracellular acidification, which mimics the tumor microenvironment[1].

Animal Model was MC38 tumor-bearing C57BL6 mice,and The dosage was 60 mg/kg.Administration was P.o.;s.c (50 mg/kg);single dose[1]

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C14H14O5S

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DMSO:50 mg/mL (169.88 mM),ultrasonic and warming and heat to 80°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years