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2’3’-c-di-AM(PS)2 (Rp,Rp)

MCE China：2’3’-c-di-AM(PS)2 (Rp,Rp)

Brand：MedChemExpress (MCE)

Cat. No.HY-12885

CAS：1638241-89-0

Synonyms：ADU-S100; MIW815; ML RR-S2 CDA

Purity：98.36%

Storage：-20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：2’3’-c-di-AM(PS)2 (Rp,Rp) (ADU-S100), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.

In Vitro：2’3’-c-di-AM(PS)2 (Rp,Rp) is unstable in its free base form. 2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt (HY-12885B) improves both stability and lipophilicity, promoting significantly increased STING signaling as compared to endogenous and pathogen-derived cyclic dinucleotides (CDNs)[1]. 2’3’-c-di-AM(PS)2 (Rp,Rp) shows enhanced type I IFN production over CDA in THP-1 human monocytes. In contrast, the dithio, mixed-linkage CDN derivatives (ML RR-CDA, ML RR-S2 CDG, and ML RR-S2 cGAMP) potently activate all five hSTING alleles, including the refractory hSTINGREF and hSTINGQ alleles. 2’3’-c-di-AM(PS)2 (Rp,Rp) 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. 2’3’-c-di-AM(PS)2 (Rp,Rp) is also found to induce aggregation of STING and induce phosphorylation of TBK1 and IRF3 in mouse bone marrow macrophage (BMM). 2’3’-c-di-AM(PS)2 (Rp,Rp) induces significantly higher levels of IFN-α when compared to ML cGAMP[1].

In Vivo：2’3’-c-di-AM(PS)2 (Rp,Rp) shows higher anti-tumor control than the endogenous ML cGAMP. A dose response of the 2’3’-c-di-AM(PS)2 (Rp,Rp) 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].

Animal Administration：Mice[1] WT C57BL/6 mice are inoculated with 5×104 B16.F10 cells in the left flank (n=8). When tumor volumes are 100 mm3 mice receive three IT doses of either ML RR-S2 CDG (25 μg), ADU-S100 (50 μg), or HBSS as control. WT C57BL/6 mice are inoculated with 5×104 B16.F10 cells in the left flank (n=5). When tumor volumes are 100 mm3 they received three IT doses of ADU-S100 at 5, 25, 50 or 100 μg or HBSS as control. WT C57BL/6 mice are inoculated with 5×104 B16.F10 cells in the left flank (n=8). When tumor volumes are 100 mm3 they receive three IT doses of 100 μg ADU-S100 or HBSS as control. Treatments are administered on days 13, 17 and 20 and tumor measurements are taken twice weekly. Results are shown as percent survival by Log-rank (Mantel-Cox) test (A and C)[1].

Cell Assay：Cryopreserved hPBMCs are thawed and 1×106 cells per well are plated in a 96 well plate in RPMI media. Cells are stimulated with 10 μM ADU-S100 or ML cGAMP for 6 hours and supernatants are harvested. Supernatants are diluted 1:2 and assayed for IFN-α protein using Cytometric Bead Array (CBA) Human Flex Set. Data is collected using a FACSVerse cytometer and analyzed by FCAP Array Software[1].

IC50 & Target：STING[1] In Vitro 2’3’-c-di-AM(PS)2 (Rp,Rp) is unstable in its free base form. 2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt (HY-12885B) improves both stability and lipophilicity, promoting significantly increased STING signaling as compared to endogenous and pathogen-derived cyclic dinucleotides (CDNs)[1]. 2’3’-c-di-AM(PS)2 (Rp,Rp) shows enhanced type I IFN production over CDA in THP-1 human monocytes. In contrast, the dithio, mixed-linkage CDN derivatives (ML RR-CDA, ML RR-S2 CDG, and ML RR-S2 cGAMP) potently activate all five hSTING alleles, including the refractory hSTINGREF and hSTINGQ alleles. 2’3’-c-di-AM(PS)2 (Rp,Rp) 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. 2’3’-c-di-AM(PS)2 (Rp,Rp) is also found to induce aggregation of STING and induce phosphorylation of TBK1 and IRF3 in mouse bone marrow macrophage (BMM). 2’3’-c-di-AM(PS)2 (Rp,Rp) induces significantly higher levels of IFN-α when compared to ML cGAMP[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> 2’3’-c-di-AM(PS)2 (Rp,Rp) Related Antibodies

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References：

[1]. Corrales L, et al. Direct Activation of STING in the Tumor Microenvironment Leads to Potent and Systemic Tumor Regression and Immunity. Cell Rep. 2015 May 19;11(7):1018-30.  [Content Brief]