MSA-2是一种口服非核苷酸STING激动剂，对人的STING亚型WT和HAQ的EC50分别为8.3和24μM。MSA-2在同基因小鼠肿瘤模型中显示抗肿瘤活性，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，并与抗PD-1协同作用。
货号:ajcx31118
CAS:129425-81-6
分子式:C14H14O5S
分子量：294.32
溶解度:DMSO: 125 mg/mL (424.71 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

MSA-2, a potent and orally available non-nucleotide STING agonist, has EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models[1].

MSA-2 dosed via either PO or SC regimens achieved comparable exposure in both tumor and plasma. MSA-2 also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes, and dosing regimens were identified that induced complete tumor regressions in 80 to 100% of treated animals[1].MSA-2 (PO: 60 mg/kg or SC: 50 mg/kg; single dose) that effectively inhibits tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor[1]. Animal Model: MC38 tumor-bearing C57BL6 mice[1]

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