| Description | MSA-2 is a potent and orally available non-nucleotide STING agonist. |
| In vivo | 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 experiments | 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] |
| molecular weight | 294.32 |
| Molecular formula | C14H14O5S |
| CAS | 129425-81-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (169.88 mM), Sonication and heating to 80℃ are recommended. |
| References | 1. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098. |