Art. -Nr.: HY-143320

STING agonist-17

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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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Reinheit: 96.15%
CAS. Nr.: 2816929-47-0
Formel: C₄₃H₅₃N₁₃O₈
Molecular Weight:879.96

Speicherung:

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

STING agonist-17 Chemical Structure

CAS. Nr.: 2816929-47-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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
T_1/2 (h)	10.54 ± 4.10
Vss (L/kg)	>17.74 ± 5.29
CL (L/h/kg)	2.12 ± 0.27
AUC_last (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.

Chemical Information

CAS. Nr. 2816929-47-0
Appearance Solid
Molecular Weight 879.96
Formel C₄₃H₅₃N₁₃O₈
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
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 (113.64 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

1.1364 mL

5.6821 mL

11.3642 mL

5 mM

0.2273 mL

1.1364 mL

2.2728 mL

10 mM

0.1136 mL

0.5682 mL

1.1364 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: 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.

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:

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 (283 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Min Jae Jeon, et al. Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor. J Med Chem. 2022 Apr 14;65(7):5407-5432. [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	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

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Heterocyclic Compound Library

Immunopotentiator 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-17

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Heterocyclic Compound Library

Immunopotentiator 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-17 Related Classifications

HY-143320 Related Classifications