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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| 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. |
| Molecular Weight | 870.00 |
| Formula | C49H55N7O8 |
| Cas No. | 3065494-66-5 |
| Smiles | C(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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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