1. Immunology/Inflammation
  2. STING
  3. ADU-S100

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

Cat. No.: HY-12885 Purity: 99.44%
Handling Instructions

ADU-S100 (MIW815), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.

For research use only. We do not sell to patients.

ADU-S100 Chemical Structure

ADU-S100 Chemical Structure

CAS No. : 1638241-89-0

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Description

ADU-S100 (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 is unstable in its free base form. ADU-S100 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].
ADU-S100 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. 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

690.54

Formula

C₂₀H₂₄N₁₀O₁₀P₂S₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 20 mg/mL (28.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4481 mL 7.2407 mL 14.4814 mL
5 mM 0.2896 mL 1.4481 mL 2.8963 mL
10 mM 0.1448 mL 0.7241 mL 1.4481 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.53%

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ADU-S100
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HY-12885
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