Art. -Nr.: HY-175714

STING agonist-46

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STING agonist-46 is an orally active STING agonist. STING agonist-46 activates the STING signaling pathway, promoting phosphorylation of TBK1 and IRF3, and secretion of IFN-β and IP-10. STING agonist-46 directly binds to STING and increases its thermal stability. STING agonist-46 demonstrates potent anti-tumor efficacy in B16F10, CT26, and 4T1 mouse models. STING agonist-46 can be used for cancer immunotherapy studies.

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Reinheit: 98.63%
CAS. Nr.: 3033532-05-4
Formel: C₁₇H₂₁NO₅S
Molecular Weight:351.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

STING agonist-46 Chemical Structure

CAS. Nr.: 3033532-05-4

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

STING agonist-46 (Compound 57) (0.37-30 μM, 24 h) exhibits potent activation on ISG pathway in THP1-Dual cells, with EC₅₀ of 2.55 μM^[1].
STING agonist-46 (10-50 μM, 24 h) shows potent activation on h-STING in THP1-Blue-ISG cells and m-STING in RAW-Lucia cells^[1].
STING agonist-46 (3.3-30 μM, 2 h) significantly promotes phosphorylation of TBK1 and IRF3 in THP1-Dual cells^[1].
STING agonist-46 (1.1-30 μM, 24 h) upregulates the expression of IFN-β and IP-10 in THP1-Dual cells^[1].
STING agonist-46 (3.3-30 μM, 48 h) activates both hSTING-R232 and hSTING-H232 subtypes in 293T-Dual reporter cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

THP1-Dual cells
Concentration:

1.1, 3.3, 10, 30 μM
Incubation Time:

24 h
Result:

Upregulated the expression of IFN-β and IP-10 in THP1-Dual cells.

In Vivo

STING agonist-46 (Compound 57) (500 μg/mouse, intratumoral injection or 100 mg/kg, p.o., days 1, 4, 7) demonstrates significant anti-tumor efficacy against B16F10/CT26/4T1 melanoma in immunocompetent mice and shows no anti-tumor efficacy against B16F10/CT26 melanoma in STING-knockout mice^[1].

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

Animal Model:

B16F10 melanoma cells (0.5 × 10⁵ in PBS)/CT26 colon tumor cells (2.5 × 10⁵ in PBS)/4T1 breast cancer cells were subcutaneously implanted into the right axilla of 6-week-old female immunocompetent WT C57BL/6 mice or STING-knockout C57BL/6 mice^[1]
Dosage:

500 μg/mouse, intratumoral injection or 100 mg/kg, p.o.
Administration:

On days 1, 4, 7
Result:

Demonstrated significant anti-tumor efficacy against B16F10/CT26/4T1 melanoma in immunocompetent mice.
Showed no anti-tumor efficacy against B16F10/CT26 melanoma in STING-knockout mice.
Showed no significant changes in body weight.

Chemical Information

CAS. Nr. 3033532-05-4
Appearance Solid
Molecular Weight 351.42
Formel C₁₇H₂₁NO₅S
Color White to light yellow
SMILES

O=C(CCC(ONC(C)C)=O)C1=CC2=CC(OC)=C(C=C2S1)OC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (284.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8456 mL

14.2280 mL

28.4560 mL

5 mM

0.5691 mL

2.8456 mL

5.6912 mL

10 mM

0.2846 mL

1.4228 mL

2.8456 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 5 mg/mL (14.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

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

Solubility: ≥ 5 mg/mL (14.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (14.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shen A, et al. Structure-Activity relationship study of benzothiophene oxobutanoic acid analogues leading to novel stimulator of interferon gene (STING) agonists. Eur J Med Chem. 2022 Nov 5;241:114627. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.8456 mL	14.2280 mL	28.4560 mL	71.1399 mL
	5 mM	0.5691 mL	2.8456 mL	5.6912 mL	14.2280 mL
	10 mM	0.2846 mL	1.4228 mL	2.8456 mL	7.1140 mL
	15 mM	0.1897 mL	0.9485 mL	1.8971 mL	4.7427 mL
	20 mM	0.1423 mL	0.7114 mL	1.4228 mL	3.5570 mL
	25 mM	0.1138 mL	0.5691 mL	1.1382 mL	2.8456 mL
	30 mM	0.0949 mL	0.4743 mL	0.9485 mL	2.3713 mL
	40 mM	0.0711 mL	0.3557 mL	0.7114 mL	1.7785 mL
	50 mM	0.0569 mL	0.2846 mL	0.5691 mL	1.4228 mL
	60 mM	0.0474 mL	0.2371 mL	0.4743 mL	1.1857 mL
	80 mM	0.0356 mL	0.1778 mL	0.3557 mL	0.8892 mL
	100 mM	0.0285 mL	0.1423 mL	0.2846 mL	0.7114 mL

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STING agonist-46

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Immunopotentiator Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

STING agonist-46

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Immunopotentiator Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

STING agonist-46 Related Classifications

HY-175714 Related Classifications