APH02174 hemiformic |
Catalog No.GC80945
One-Click Copy Product Info
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APH02174 hemiformic is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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In Vivo, APH02174 (10-100 mg/kg; p.o.; twice daily; for 7 days) hemiformic reduces imiquimod-induced psoriasis-like skin inflammation significantly degrades the IRAK4 protein level in the spleen of the Imiquimod (IMQ) induced mice[1]. APH02174 (30-100 mg/kg; p.o.; once daily; for 14 days) hemiformic significantly improves arthritis in the rheumatoid arthritis mice[1].
In Vitro, APH02174 (0.24-1000 nM) hemiformic can selectively degrade IRAK4 protein in various cells, including THP-1 (DC50 = 4.01 nM), hPBMCs (DC50 = 0.43 nM) and mouse PBMCs (DC50 = 3.57 nM) [1]. APH02174 (0.03-2000 nM; 24 h) hemiformic significantly inhibits the Lipopolysaccharides (LPS) induced IL-6 release in the hPBMCs (IC50 = 16.43 nM) [1].
References:
[1]. Wu XW, et al. Discovery of APH02174 as a Highly Selective and Orally Bioavailable IRAK4 Degrader for the Treatment of Inflammatory Diseases. J Med Chem. 2025 Jun 26;68(12):12845-12861.
| Cas No. | SDF | ||
| Formula | C49H55N7O8·1/2CH2O2 | M.Wt | 916.03 |
| Solubility | Storage | Store at 4°C, away from moisture | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.0917 mL | 5.4583 mL | 10.9167 mL |
| 5 mM | 218.3 μL | 1.0917 mL | 2.1833 mL |
| 10 mM | 109.2 μL | 545.8 μL | 1.0917 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)