MSA-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MSA-2 是一种有效的口服非核苷酸 STING 激动剂，对人 STING 亚型 WT 和 HAQ 的 EC50 值分别为 8.3 和 24 μM。

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.

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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.

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Immunology/Inflammation

STING

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129425-81-6

294.32

O=C(C1=CC(C(S1)=C2)=CC(OC)=C2OC)CCC(O)=O

>98% (HPLC)

DMSO : 50 mg/mL (169.88 mM; ultrasonic and warming and heat to 80°C)

O=C(C1=CC(C(S1)=C2)=CC(OC)=C2OC)CCC(O)=O

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(-20℃)

With Ice Pack

≥ 2 years