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diABZI STING agonist-1 trihydrochloride

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Catalog No. T5516Cas No. 2138299-34-8

diABZI STING agonist-1 (trihydrochloride) is a stimulator of interferon genes (STING) receptor agonist.

diABZI STING agonist-1 trihydrochloride

diABZI STING agonist-1 trihydrochloride

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Purity: 99.55%
Catalog No. T5516Cas No. 2138299-34-8
diABZI STING agonist-1 (trihydrochloride) is a stimulator of interferon genes (STING) receptor agonist.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$158In StockIn Stock
2 mg$218In StockIn Stock
5 mg$335In StockIn Stock
10 mg$533In StockIn Stock
25 mg$786In StockIn Stock
50 mg$1,230-In Stock
100 mg$1,660-In Stock
200 mg$2,230-In Stock
1 mL x 10 mM (in DMSO)$591In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.55%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
diABZI STING agonist-1 (trihydrochloride) is a stimulator of interferon genes (STING) receptor agonist.
Targets&IC50
STING (mouse):200 ng /mL (EC50), STING (human):130 nM (EC50), H69AR cells:0.035 μM (EC50)
In vitro
diABZI STING agonist-1 trihydrochloride is a selective stimulator of interferon genes receptor (STING) agonist with EC50 values ​​of 130 and 186 nM in humans and mice.
In vivo
METHODS: diABZI STING agonist-1 (trihydrochloride) (3mg/kg, intravenous injection) was administered to BALB/c mice to observe the pharmacokinetic spectrum in the mice.
RESULTS diABZI STING agonist-1 (trihydrochloride) was systematically exposed, with a half-life of 1.4 h, and the systemic concentration was greater than the half-maximum effective concentration (EC50) of mouse STING (200 ng/ml). [1]
METHODS: diABZI STING agonist-1 (trihydrochloride) (1.5 mg/kg, 1, 4 and 8 days, intravenous injection) in mice with subcutaneous CT-26 tumors was analyzed by tumor volume AUC.
RESULTS diABZI STING agonist-1 (trihydrochloride) had a significant inhibitory effect on tumor growth and significantly improved survival rate (P<0.001). [1]
Animal Research
To evaluate the potential therapeutic effects of systemically administered diABZI STING agonist-1 trihydrochloride, tested the efficacy of intravenously delivered diABZI STING in a syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice.?We first established the pharmacokinetic profile of STING in BALB/c mice following intravenous injection of 3 mg/kg .?STING exhibited systemic exposure with a half-life of 1.4 h and achieved systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (~200 ng/ml).?Next, we tested an intermittent dosing paradigm in which 1.5 mg/kg STING was injected intravenously on days 1, 4, and 8 in mice with approximately 100 mm^3 subcutaneous CT-26 tumours.?Treatment with STING resulted in significant tumour growth inhibition as measured by tumour volume AUC analysis (P<0.001), and significantly improved survival (P<0.001) with 8 out of 10 mice remaining tumour free at the end of the study on day 43.
Chemical Properties
Molecular Weight959.32
FormulaC42H54Cl3N13O7
Cas No.2138299-34-8
SmilesCl.Cl.Cl.CCn1nc(C)cc1C(=O)Nc1nc2cc(cc(OC)c2n1C\C=C\Cn1c(NC(=O)c2cc(C)nn2CC)nc2cc(cc(OCCCN3CCOCC3)c12)C(N)=O)C(N)=O
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 5 mg/mL (5.21 mM), Sonication is recommended.
DMSO: 15 mg/mL (15.64 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.08 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM1.0424 mL5.2120 mL10.4241 mL52.1203 mL
5 mM0.2085 mL1.0424 mL2.0848 mL10.4241 mL
DMSO
1mg5mg10mg50mg
10 mM0.1042 mL0.5212 mL1.0424 mL5.2120 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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