2. Immunology/Inflammation
  3. STING
  4. STING agonist-17

STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization.

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STING agonist-17 Chemical Structure

STING agonist-17 Chemical Structure

CAS No. : 2816929-47-0

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Based on 1 publication(s) in Google Scholar

STING agonist-17 Related Antibodies

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Description

STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization[1].

IC50 & Target

IC50=0.062 nM
In Vitro

STING agonist-17 (compound 4a) inhibits the activity of four major CYP isozymes (CYP1A2, CYP2C9, CYP2C19 and CYP2D6) with IC50 values > 100 μM and for CYP3A4 with an IC50 = 4.2 μM[1].
STING agonist-17 (compound 4a) (0-2 μM, 24 hours) induces IFN-β secretion with the EC50 of 2.0 nM[1].
STING agonist-17 (compound 4a) (2 nM, 10 nM, 6 hours) can induce the expression of signal transduction factors[1].
The pharmacokinetic parameters of Compound 4a in vitro[1].

Parameter Compound 4a
CYP inhibition (IC50, μM)
1A2 >100.0
2C9 >100.0
2C19 >100.0
2D6 >100.0
3A4 4.2
Cardiotoxicity (IC50, μM)
hERG patch clamp assay >50.0
Liver microsomal phase I stability
mouse (%) 38.7 ± 2.6
human (%) 11.2 ± 2.7
Plasma stability
mouse (%) >99
human (%) >99

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

STING agonist-17 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 dual cells
Concentration: 2 nM, 10 nM
Incubation Time: 6 hours
Result: Induced phosphorylation of signal transduction factors STING、TBK1、IRF3 and STAT1 at 2 nM.
Activated the expression of IFNB gene and IFN stimulated gene (ISG).
In Vivo

STING agonist-17 (compound 4a) (Intravenous injection; 0.015 mg/kg, 1.5 mg/kg; every other day; a week) has an inhibitory effect on tumor growth in CT26 cells-derived colon carcinoma female BALB/c mice[1].
The pharmacokinetic parameters of Compound 4a in vivo[1].

Parameter Compound 4a
T1/2 (h) 10.54 ± 4.10
Vss (L/kg) >17.74 ± 5.29
CL (L/h/kg) 2.12 ± 0.27
AUClast (μg•h/mL) 4.20 ± 0.26
AUC∞ (μg•h/mL) >4.78 ± 0.59

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

Animal Model: Female BALB/c mice aged 6 weeks[1]
Dosage: 0.015 mg/kg, 1.5 mg/kg
Administration: Intravenous injection; every other day; a week
Result: Inhibited tumor growth in both doses and caused 57% inhibition at a concentration of 1.5 mg/kg on the 17th day without weight loss.
Molecular Weight

879.96

Formula

C43H53N13O8
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CCN1N=C(C=C1C(NC2=NC3=C(N2C/C=C/CN4C(NC(C5=CC(C)=NN5CC)=O)=NC6=CC(C(N)=O)=CC(OCCCNC(OC(C)(C)C)=O)=C64)C(OC)=CC(C(N)=O)=C3)=O)C
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 : 100 mg/mL (113.64 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 1.1364 mL 5.6821 mL 11.3642 mL
5 mM 0.2273 mL 1.1364 mL 2.2728 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. 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: 2.5 mg/mL (2.84 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: 2.5 mg/mL (2.84 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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).
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. 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 1.1364 mL 5.6821 mL 11.3642 mL 28.4104 mL
5 mM 0.2273 mL 1.1364 mL 2.2728 mL 5.6821 mL
10 mM 0.1136 mL 0.5682 mL 1.1364 mL 2.8410 mL
15 mM 0.0758 mL 0.3788 mL 0.7576 mL 1.8940 mL
20 mM 0.0568 mL 0.2841 mL 0.5682 mL 1.4205 mL
25 mM 0.0455 mL 0.2273 mL 0.4546 mL 1.1364 mL
30 mM 0.0379 mL 0.1894 mL 0.3788 mL 0.9470 mL
40 mM 0.0284 mL 0.1421 mL 0.2841 mL 0.7103 mL
50 mM 0.0227 mL 0.1136 mL 0.2273 mL 0.5682 mL
60 mM 0.0189 mL 0.0947 mL 0.1894 mL 0.4735 mL
80 mM 0.0142 mL 0.0710 mL 0.1421 mL 0.3551 mL
100 mM 0.0114 mL 0.0568 mL 0.1136 mL 0.2841 mL
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STING agonist-17 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-172816929-47-0STING agonist17STING agonist 17STINGStimulator of Interferon GenesTMEM173MITAERISMPYSSTING agonist，cancerInhibitorinhibitorinhibit

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