1638241-89-0
- CAS号:1638241-89-0
- 英文名:STING-Inducer-1
- 中文名:1638241-89-0
- CBNumber:CB13041465
- 分子式:C20H24N10O10P2S2
- 分子量:690.54
- MOL File:1638241-89-0.mol
- 沸点 :1020.8±75.0 °C(Predicted)
- 密度 :2.43±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO : 2 mg/mL (2.90 mM)
- 形态 :Solid
- 酸度系数(pKa) :-0.67±0.70(Predicted)
- 颜色 :White to off-white
- InChIKey :IZJJFUQKKZFVLH-UUXHIKLWNA-N
1638241-89-0性质、用途与生产工艺
- 生物活性 ADU-S100 (MIW815) 是干扰素基因刺激物的激活剂 (STING),具有有效的抗肿瘤和免疫活性。
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靶点
STING
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体外研究
ADU-S100 shows enhanced type I IFN production over CDA in THP-1 human monocytes. In contrast, the dithio, mixed-linkage cyclic dinucleotide (CDN) derivatives (ML RR-CDA, ML RR-S2 CDG, and ML RR-S2 cGAMP) potently activate all five hSTING alleles, including the refractory hSTING REF and hSTING Q alleles. ADU-S100 induces the highest expression of IFN-β and the pro-inflammatory cytokines TNF-α, IL-6, and MCP-1 on a molar equivalent basis, as compared to endogenous ML cGAMP and the TLR3 agonist poly I:C. ADU-S100 is also found to induce aggregation of STING and induce phosphorylation of TBK1 and IRF3 in mouse bone marrow macrophage (BMM). ADU-S100 induces significantly higher levels of IFN-α when compared to ML cGAMP.
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体内研究
ADU-S100 shows higher anti-tumor control than the endogenous ML cGAMP. A dose response of the ADU-S100 compound is performed in B16 tumor-bearing mice, which identifies an optimal antitumor dose level that also elicites maximum tumor antigen-specific CD8 + T cell responses, and improves long-term survival to 50%.
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