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

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

Cat. No.: HY-12885B Purity: 99.23%
Handling Instructions

ADU-S100 ammonium salt (ML RR-S2 CDA ammonium salt; MIW815 ammonium salt), 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 ammonium salt Chemical Structure

ADU-S100 ammonium salt Chemical Structure

CAS No. : 1638750-96-5

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10 mM * 1 mL in DMSO USD 1028 In-stock
Estimated Time of Arrival: December 31
1 mg USD 195 In-stock
Estimated Time of Arrival: December 31
5 mg USD 645 In-stock
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10 mg USD 1150 In-stock
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25 mg USD 2400 In-stock
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50 mg USD 4200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

ADU-S100 ammonium salt (ML RR-S2 CDA ammonium salt; MIW815 ammonium salt), 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 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].

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].

Clinical Trial
Molecular Weight

724.60

Formula

C₂₀H₃₀N₁₂O₁₀P₂S₂

CAS No.

1638750-96-5

SMILES

OC1([H])[[email protected]](O[[email protected]]([S-])(OC[[email protected]](O[[email protected]@H](N2C3=NC=NC(N)=C3N=C2)[[email protected]@H]4O)([H])[[email protected]@]4([H])O5)=O)([H])[[email protected]](N6C7=NC=NC(N)=C7N=C6)O[[email protected]]1([H])CO[[email protected]]5([S-])=O.[NH4+].[NH4+]

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: 

DMSO : 15 mg/mL (20.70 mM; Need ultrasonic and warming)

H2O : 12.5 mg/mL (17.25 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3801 mL 6.9004 mL 13.8007 mL
5 mM 0.2760 mL 1.3801 mL 2.7601 mL
10 mM 0.1380 mL 0.6900 mL 1.3801 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 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].

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).

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

References

Purity: 99.23%

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ADU-S100 ammonium salt
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