ADU-S100

1638241-89-0

C20H24N10O10P2S2

DMSO : 2 mg/mL (2.90 mM; Need ultrasonic)

Immunology/Inflammation

ADU-S100 (ML RR-S2 CDA; MIW815), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity^[1]. IC50 & Target: STING^[1] In Vitro: 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-beta and the pro-inflammatory cytokines TNF-alpha, 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-alpha when compared to ML cGAMP^[1]. In Vivo: 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%^[1].