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

MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide.

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MSA-2 dimer Chemical Structure

MSA-2 dimer Chemical Structure

CAS No. : 2377881-92-8

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Based on 1 publication(s) in Google Scholar

MSA-2 dimer Related Antibodies

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  • Purity & Documentation

  • References

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Description

MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1].

IC50 & Target

Kd: 145 μM (STING)[1]
In Vivo

MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1].
MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1].
MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors[1].
MSA-2 dimer (60 mg/kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues [1].
MSA-2 dimer (THP-1 cells) induces phosphorylation of both TBK1 and IR. MSA-2 dimer (10 μM and 33 μM; macrophages) induces IFN-β[1].
MSA-2 dimer also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes[1].

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

Animal Model: B16F10 tumor-bearing mice
Dosage: 60 mg/kg
Administration: P.o.; 50 days
Result: Inhibited tumor growth and prolonged overall survival.
Animal Model: C57BL6 mice
Dosage: 40 mg/kg
Administration: S.c.; 25 days
Result: Induced complete tumor regression.
Animal Model: C57BL6 mice
Dosage: 60 mg/kg
Administration: P.o.; 4 hours
Result: Increased proinflammatory cytokine (IFN-β) level in tumors.
Animal Model: C57BL6 mice
Dosage: 50 mg/kg
Administration: S.c.; 4 hours
Result: MSA-2 concentrations were observed in tumors than in plasma or other nontumor tissues.
Molecular Weight

568.66

Formula

C29H28O8S2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(CCC(C1=CC2=C(C=C(C(CCCC3=CC4=C(C=C3OC)SC(C(CCC(O)=O)=O)=C4)=C2)OC)S1)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 70 mg/mL (123.10 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 1.7585 mL 8.7926 mL 17.5852 mL
5 mM 0.3517 mL 1.7585 mL 3.5170 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 1.75 mg/mL (3.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.5 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: 1.75 mg/mL (3.08 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.5 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 (sealed storage, away from moisture)

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: 99.30%

COA (244 KB) HNMR (413 KB) LCMS (113 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 1.7585 mL 8.7926 mL 17.5852 mL 43.9630 mL
5 mM 0.3517 mL 1.7585 mL 3.5170 mL 8.7926 mL
10 mM 0.1759 mL 0.8793 mL 1.7585 mL 4.3963 mL
15 mM 0.1172 mL 0.5862 mL 1.1723 mL 2.9309 mL
20 mM 0.0879 mL 0.4396 mL 0.8793 mL 2.1982 mL
25 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7585 mL
30 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4654 mL
40 mM 0.0440 mL 0.2198 mL 0.4396 mL 1.0991 mL
50 mM 0.0352 mL 0.1759 mL 0.3517 mL 0.8793 mL
60 mM 0.0293 mL 0.1465 mL 0.2931 mL 0.7327 mL
80 mM 0.0220 mL 0.1099 mL 0.2198 mL 0.5495 mL
100 mM 0.0176 mL 0.0879 mL 0.1759 mL 0.4396 mL
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MSA-2 dimer 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-2 dimer2377881-92-8STINGStimulator of Interferon GenesTMEM173MITAERISMPYSSelectiveOralNon-nucleotideTHP-1AntitumorImmunogenicDimerInhibitorinhibitorinhibit

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