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APH02174

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Catalog No. T211447Cas No. 3065494-66-5

APH02174 is a highly selective and orally active IRAK4PROTAC degrader, with a DC50 of 4.01 nM in THP-1 cells. It blocks inflammatory signaling by inhibiting IL-6 release and is applicable for researching inflammatory diseases such as psoriasis and rheumatoid arthritis.

APH02174

APH02174

Copy Product Info
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Catalog No. T211447Cas No. 3065494-66-5
APH02174 is a highly selective and orally active IRAK4PROTAC degrader, with a DC50 of 4.01 nM in THP-1 cells. It blocks inflammatory signaling by inhibiting IL-6 release and is applicable for researching inflammatory diseases such as psoriasis and rheumatoid arthritis.
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
APH02174 is a highly selective and orally active IRAK4PROTAC degrader, with a DC50 of 4.01 nM in THP-1 cells. It blocks inflammatory signaling by inhibiting IL-6 release and is applicable for researching inflammatory diseases such as psoriasis and rheumatoid arthritis.
Targets&IC50
IRAK4:4.01 nM (DC50)
In vitro
APH02174, in the concentration range of 0.24-1000 nM, selectively degrades IRAK4 protein in various cells, including THP-1 (DC50 = 4.01 nM), hPBMCs (DC50 = 0.43 nM), and mouse PBMCs (DC50 = 3.57 nM). Additionally, at 0.03-2000 nM for 24 hours, APH02174 significantly inhibits LPS-induced IL-6 release in hPBMCs with an IC50 of 16.43 nM.
In vivo
APH02174 administered orally at doses of 10-100 mg/kg twice daily for 7 days can reduce skin inflammation induced by IMQ and degrade IRAK4 protein levels in the spleen of psoriatic mice. Additionally, APH02174 at 30 or 100 mg/kg once daily for 14 days significantly alleviates arthritis in rheumatoid arthritis mouse models.
Chemical Properties
Molecular Weight870.00
FormulaC49H55N7O8
Cas No.3065494-66-5
SmilesC(N1CCC2(CC=3C(O2)=CC(=C(NC(=O)C=4C=5C(OC4)=CC=CN5)C3)N6CCC(CO)CC6)CC1)[C@H]7CC[C@H](OCC#CC8=C9C(N(C(=O)N9C)C%10C(=O)NC(=O)CC%10)=CC=C8)CC7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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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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
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