2. Immunology/Inflammation
  3. STING
  4. MSA-2

MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.

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MSA-2 Chemical Structure

MSA-2 Chemical Structure

CAS No. : 129425-81-6

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10 mM * 1 mL in DMSO
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Based on 10 publication(s) in Google Scholar

MSA-2 Related Antibodies

Top Publications Citing Use of Products

    MSA-2 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2022 Oct 24;12(1):17827.  [Abstract]

    Both diABZI (100 nM) and MSA-2 (25 µM) readily trigger the cleavage of caspase-3 and PARP-1 in monocytes. Low dose of MSA-2 (2.5 µM) and diABZI (100 nM) lead to the cleavage of gasdermin D (an indicator of pyroptosis) in monocytes.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models[1][2].

    In Vivo

    MSA-2 dosed via either PO or SC regimens achieved comparable exposure in both tumor and plasma. MSA-2 also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes, and dosing regimens were identified that induced complete tumor regressions in 80 to 100% of treated animals[1].
    MSA-2 (PO: 60 mg/kg or SC: 50 mg/kg; single dose) that effectively inhibits tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor[1].

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

    Animal Model: MC38 tumor-bearing C57BL6 mice[1]
    Dosage: 60 mg/kg
    Administration: P.o. ; s.c (50 mg/kg); single dose
    Result: PO or SC doses of MSA-2 that effectively inhibited tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor.
    Molecular Weight

    294.32

    Formula

    C14H14O5S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to brown

    SMILES

    O=C(C1=CC(C(S1)=C2)=CC(OC)=C2OC)CCC(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (169.88 mM; Need ultrasonic; 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 3.3977 mL 16.9883 mL 33.9766 mL
    5 mM 0.6795 mL 3.3977 mL 6.7953 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, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 2.08 mg/mL (7.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 25 mg/mL (84.94 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  1% (w/v) carboxymethylcellulose (CMC)

      Solubility: 5 mg/mL (16.99 mM); Suspended solution; Need ultrasonic

    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, 2 years; -20°C, 1 year (protect from light)

    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

    Purity: 99.64%

    COA (247 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3977 mL 16.9883 mL 33.9766 mL 84.9416 mL
    5 mM 0.6795 mL 3.3977 mL 6.7953 mL 16.9883 mL
    10 mM 0.3398 mL 1.6988 mL 3.3977 mL 8.4942 mL
    15 mM 0.2265 mL 1.1326 mL 2.2651 mL 5.6628 mL
    20 mM 0.1699 mL 0.8494 mL 1.6988 mL 4.2471 mL
    25 mM 0.1359 mL 0.6795 mL 1.3591 mL 3.3977 mL
    30 mM 0.1133 mL 0.5663 mL 1.1326 mL 2.8314 mL
    40 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1235 mL
    50 mM 0.0680 mL 0.3398 mL 0.6795 mL 1.6988 mL
    60 mM 0.0566 mL 0.2831 mL 0.5663 mL 1.4157 mL
    80 mM 0.0425 mL 0.2124 mL 0.4247 mL 1.0618 mL
    100 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8494 mL
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    MSA-2 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:

    MSA-2129425-81-6MSA2MSA 2STINGStimulator of Interferon GenesTMEM173MITAERISMPYSinterferon-βsecretionimmunityMC38tumorTNF-αInhibitorinhibitorinhibit

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