| 产品描述: | MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models |
| 靶点: |
STING |
| 体内研究: |
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. 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. Animal Model: MC38 tumor-bearing C57BL6 mice Dosage: 60 mg/kg Administration: P.o. ; s.c (50 mg/kg); single dose Result: PO or SC doses of MSA-2 that effectively inhibited tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor. |
| 参考文献: |
1. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098.
2. Liu J, et al. Identification of MSA-2: An oral antitumor non-nucleotide STING agonist. Signal Transduct Target Ther. 2021;6(1):18. Published 2021 Jan 12. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.398 ml |
16.988 ml |
33.977 ml |
| 5 mM |
0.68 ml |
3.398 ml |
6.795 ml |
| 10 mM |
0.34 ml |
1.699 ml |
3.398 ml |
| 50 mM |
0.068 ml |
0.34 ml |
0.68 ml |
|
| 注意: |
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