2. Immunology/Inflammation
  3. STING
  4. STING agonist-3 trihydrochloride

STING agonist-3 trihydrochloride 

Cat. No.: HY-103665A Purity: 98.36%
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STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

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

STING agonist-3 trihydrochloride Chemical Structure

STING agonist-3 trihydrochloride Chemical Structure

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Based on 9 publication(s) in Google Scholar

Other Forms of STING agonist-3 trihydrochloride:

STING agonist-3 trihydrochloride Related Antibodies

Top Publications Citing Use of Products

    STING agonist-3 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2022 Oct;610(7933):761-767.  [Abstract]

    Incubate HeLa cGAS KO cells with NC siRNA or siRNAs targeting AP-1σ1 and AP-1 σ3 for 3 days and reconstitute with empty vector or HA-tagged AP-1σ1 are treated with 2.5 µM diABZI (STING agonist-3) for 0, 2, 4 h before analysis by western blot.

    STING agonist-3 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2022 Oct;610(7933):761-767.  [Abstract]

    STING and pSTING are enriched in CCVs obtained from STING agonist-3 (diABZI; 2.5 μM; for 2 hours)-stimulated cells, but not in those obtained from unstimulated cells.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer[1].

    IC50 & Target

    STING[1]
    In Vitro

    STING agonist-3 trihydrochloride exhibits a pEC50 value of 7.5 in activation of STING in cells, this assay is determined using a luciferase reporter assay in human embryonic kidney cells (HEK293T) co-transfected with plasmids expressing STING and the enzyme firefly luciferase driven by the interferon stimulated response element promoter[1].
    STING agonist-3 trihydrochloride exhibits a pIC50 value of 9.5 in FRET assay. This is a competition binding assay which aims to determine the binding potency of molecules to the C-terminal Domain (CTD) of human STING[1].

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

    STING agonist-3 trihydrochloride Related Antibodies
    Molecular Weight

    860.19

    Formula

    C37H45Cl3N12O6
    Appearance

    Solid

    SMILES

    O=C(N)C1=CC=C(N(C(NC(C2=CC(C)=NN2CC)=O)=N3)C/C=C/CN4C5=C(N=C4NC(C6=CC(C)=NN6CC)=O)C=C(C(N)=O)C=C5OCCCO)C3=C1.Cl.Cl.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light, stored under nitrogen

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 20 mg/mL (23.25 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1625 mL 5.8127 mL 11.6253 mL
    5 mM 0.2325 mL 1.1625 mL 2.3251 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2 mg/mL (2.33 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2 mg/mL (2.33 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.1625 mL 5.8127 mL 11.6253 mL 29.0633 mL
    5 mM 0.2325 mL 1.1625 mL 2.3251 mL 5.8127 mL
    10 mM 0.1163 mL 0.5813 mL 1.1625 mL 2.9063 mL
    15 mM 0.0775 mL 0.3875 mL 0.7750 mL 1.9376 mL
    20 mM 0.0581 mL 0.2906 mL 0.5813 mL 1.4532 mL
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    STING agonist-3 trihydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    STING agonist-3 trihydrochlorideSTINGStimulator of Interferon GenesTMEM173MITAERISMPYScancertumorInhibitorinhibitorinhibit

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