Zabedosertib
Based on 2 publication(s) in Google Scholar
Zabedosertib (BAY 1834845) is a selective, orally active IRAK4 inhibitor with immunomodulatory potential, IC50 is 3.55 nM. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors. Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation.
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- Purity: 98.22%
- CAS No.: 1931994-81-8
- 화학식: C20H21F3N4O4S
- 분자량:470.47
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Zabedosertib
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Biological Activity
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IRAK4 3.55 nM (IC50) |
Zabedosertib inhibits IL-β(p.o., 40-80 mg/kg, once), LPS (p.o., 10-40 mg/kg, once) and Imiquimod (p.o., 15-150 mg/kg, twice daily for 7 days) induced inflammation[3].
Zabedosertib has a Pharmacokinetic profile in rats[3]:
Pharmacokinetic Analysis of Zabedosertib in rats[1]
| species | Doseiv (mg/kg) | AUCnorm,iv (kg·h/L) | CLblood (L/h/kg) | Vss (L/kg) | T1/2,iv (h) | Dosepo(mg/kg) | AUCnorm,po (kg·h/L)) | Cmax,norm (kg/L) | Tmax (h) | F (%) |
| rat | 0.5 | 5.6 | 0.24 | 0.92 | 4.2 | 2.0 | 5.3 | 0.55 | 4.0 | 94 |
| dog | 0.5 | 15 | 0.088 | 1.6 | 17 | 1.0 | 15 | 0.57 | 2.0 | 104 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS induced ARDS in BLAB/c mice[2]
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Dosage:150 mg/kg
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Administration:p.o., twice (30 min before and 6 h after LPS-injection or 4 h and 12 h after LPS-injection)
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Result:Decreased inflammatory cells infiltration.
Combination of Zabedosertib and DEX ( HY-14648) decreased T-cells, monocytes and macrophages.
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Animal Model:BALB/c mice[3]
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Dosage:IL-β:40-80 mg/kg, LPS: 10-40 mg/kg, Imiquimod: 15-150 mg/kg
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Administration:oral gavage, IL-β: once, LPS: once, Imiquimod: twice daily for 7 days
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Result:Inhibited IL-β, LPS induced inflammation in a dose-dependent manner. Inhibited Imiquimod induced inflammation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1931994-81-8
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Appearance Solid
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분자량 470.47
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화학식 C20H21F3N4O4S
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Color White to off-white
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SMILES
O=C(C1=CC=CC(C(F)(F)F)=N1)NC2=CC3=CN(CCS(=O)(C)=O)N=C3C=C2C(C)(C)O
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Synonyms
BAY 1834845
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Exp Eye Res
Proanthocyanidins inhibit the inflammation response of dry eye by regulating IRAK4/JAK1/STAT1 signaling pathway. [Abstract]2026 May:266:110936. PMID: 41724228 -
Microbes Infect
USP13-mediated IRAK4 deubiquitination disrupts the pathological symptoms of lipopolysaccharides-induced sepsis. [Abstract]2021 Nov-Dec;23(9-10):104867. PMID: 34298177
용액&용해도
DMSO : 125 mg/mL (265.69 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[2]. Li Q, et al., Oral IRAK4 inhibitor BAY-1834845 prevents acute respiratory distress syndrome. Biomed Pharmacother. 2022 Sep;153:113459. [Content Brief]
[3]. Bothe U, et al., Discovery of IRAK4 Inhibitors BAY1834845 (Zabedosertib) and BAY1830839. J Med Chem. 2024 Jan 25;67(2):1225-1242. [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1255 mL | 10.6277 mL | 21.2553 mL | 53.1384 mL |
| 5 mM | 0.4251 mL | 2.1255 mL | 4.2511 mL | 10.6277 mL | |
| 10 mM | 0.2126 mL | 1.0628 mL | 2.1255 mL | 5.3138 mL | |
| 15 mM | 0.1417 mL | 0.7085 mL | 1.4170 mL | 3.5426 mL | |
| 20 mM | 0.1063 mL | 0.5314 mL | 1.0628 mL | 2.6569 mL | |
| 25 mM | 0.0850 mL | 0.4251 mL | 0.8502 mL | 2.1255 mL | |
| 30 mM | 0.0709 mL | 0.3543 mL | 0.7085 mL | 1.7713 mL | |
| 40 mM | 0.0531 mL | 0.2657 mL | 0.5314 mL | 1.3285 mL | |
| 50 mM | 0.0425 mL | 0.2126 mL | 0.4251 mL | 1.0628 mL | |
| 60 mM | 0.0354 mL | 0.1771 mL | 0.3543 mL | 0.8856 mL | |
| 80 mM | 0.0266 mL | 0.1328 mL | 0.2657 mL | 0.6642 mL | |
| 100 mM | 0.0213 mL | 0.1063 mL | 0.2126 mL | 0.5314 mL |
Zabedosertib Related Classifications
HY-139374 Related Classifications
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