货号:A1365634 同义名: 5,6-dimethoxy-γ-oxo-benzo[b]thiophene-2-Butanoic Acid
MSA-2是一种 STING 激动剂,具有抗肿瘤活性,并可能与抗 PD-1 治疗联合使用。
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描述 | MSA-2, a powerful orally available non-nucleotide STING agonist, binds to STING as a noncovalent dimer with nanomolar affinity. It displays EC50 values of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 promotes interferon-β secretion in tumors, leads to tumor regression with lasting antitumor immunity, and enhances the effectiveness of anti-PD-1 therapy in syngeneic mouse tumor models[1][2]. |
体内研究 | MSA-2, administered either orally (PO) or subcutaneously (SC), achieves similar levels of exposure in both tumor and plasma. Additionally, MSA-2 demonstrates dose-dependent antitumor effects whether delivered intratumorally (IT), subcutaneously (SC), or orally (PO). Dosing regimens have been established that result in complete tumor regression in 80 to 100% of the animals treated[1]. MSA-2 (PO: 60 mg/kg or SC: 50 mg/kg; single dose) effectively inhibits tumor growth and significantly increases levels of IFN-β, interleukin-6 (IL-6), and TNF-α within the tumor[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.40mL 0.68mL 0.34mL |
16.99mL 3.40mL 1.70mL |
33.98mL 6.80mL 3.40mL |
CAS号 | 129425-81-6 |
分子式 | C14H14O5S |
分子量 | 294.323 |
别名 | 5,6-dimethoxy-γ-oxo-benzo[b]thiophene-2-Butanoic Acid |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(169.88 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |