2. Immunology/Inflammation
  3. IRAK
  4. Zabedosertib

Zabedosertib  (Synonyms: BAY 1834845)

Cat. No.: HY-139374 Purity: 98.14%
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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.

For research use only. We do not sell to patients.

Zabedosertib Chemical Structure

Zabedosertib Chemical Structure

CAS No. : 1931994-81-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 198 In-stock
Solid
5 mg USD 180 In-stock
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50 mg USD 960 In-stock
100 mg USD 1550 In-stock
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Based on 1 publication(s) in Google Scholar

Zabedosertib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Zabedosertib

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IRAK1 IRAK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1]. Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation[2].

IC50 & Target

IRAK4

3.55 nM (IC50)

In Vitro

Zabedosertib decreases inflammatory cytokines secretion (500 nM), such as IL-1, IFN-γ, TNF-α, and IL-17[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Zabedosertib Related Antibodies
In Vivo

Zabedosertib (150 mg/kg, p.o., twice) prevents lung injury and reduces inflammation in LPS induced ARDS in BALB/c mice[2].
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.

Animal Model: LPS induced ARDS in BLAB/c mice[2]
Dosage: 150 mg/kg
Administration: p.o., twice (30 min before and 6 h after LPS-injection or 4 h and 12 h after LPS-injection)
Result: Decreased inflammatory cells infiltration.
Combination of Zabedosertib and DEX ( HY-14648) decreased T-cells, monocytes and macrophages.
Animal Model: BALB/c mice[3]
Dosage: IL-β:40-80 mg/kg, LPS: 10-40 mg/kg, Imiquimod: 15-150 mg/kg
Administration: oral gavage, IL-β: once, LPS: once, Imiquimod: twice daily for 7 days
Result: Inhibited IL-β, LPS induced inflammation in a dose-dependent manner. Inhibited Imiquimod induced inflammation.
Clinical Trial
Molecular Weight

470.47

Formula

C20H21F3N4O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC(C(F)(F)F)=N1)NC2=CC3=CN(CCS(=O)(C)=O)N=C3C=C2C(C)(C)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1255 mL 10.6277 mL 21.2553 mL
5 mM 0.4251 mL 2.1255 mL 4.2511 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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
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Zabedosertib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zabedosertib1931994-81-8BAY 1834845BAY1834845BAY-1834845IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseIRAK4inflammationARDSIL-βLPSImiquimodInhibitorinhibitorinhibit

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