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2’3’-c-di-AM(PS)2 (Rp,Rp) disodium salt

MCE China：2’3’-c-di-AM(PS)2 (Rp,Rp) disodium salt

Brand：MedChemExpress (MCE)

Cat. No.HY-12885A

CAS：1638750-95-4

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

Purity：99.43%

Storage：-20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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

Description：2’3’-c-di-AM(PS)2 (Rp,Rp) disodium salt (ADU-S100 disodium salt) is an activator of stimulator of interferon genes (STING).

In Vitro：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 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 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 supplemented with 10% FBS, 1% non-essential amino acids, 1% penicillin/streptomycin, L-glutamine, 10 mM HEPES buffer, 1 mM Sodium Pyruvate, 0.055 mM β-ME at 37°C with 5% CO2. 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) 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 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) disodium salt 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]