Zunsemetinib
Based on 1 Customer Validation
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 1640282-42-3
- Formula: C25H22ClF2N5O3
- Molecular Weight:513.92
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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MAPK Compound Library
HY-L010
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Clinical Compound Library
HY-L026
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Drug Repurposing Compound Library
HY-L035
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Oxygen Sensing Compound Library
HY-L045
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Pyroptosis Compound Library
HY-L059
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
MK2[1]
Zunsemetinib (1 and 10 μM; 1 hour; WT and NOM ID BMMs) has no effect on NLRP3 expression, but decreases IL-1β expression by promoting IL-1β mRNA degradation[1].
Zunsemetinib (0.4 nM-1 μM; 16 hours; PBMC) reduces IL-1β secretion and promotes IL-1β mRNA instability[1].
Zunsemetinib selectively blocks p38α MAPK activation of the proinflammatory kinase MK2 while sparing p38α activation of other effectors such as PRAK and ATF2. Zunsemetinib inhibits in vitro osteoclast formation induced by RANKL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:WT and NOM ID BMMs
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Concentration:1 and 10 μM
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Incubation Time:1 hour
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Result:Had no effect on NLRP3 expression, but decreased IL-1β expression by promoting IL-1β mRNA degradation.
Zunsemetinib (10 and 20 mg/kg; p.o.) increases bone density[1].
Zunsemetinib prevents osteopenia in NOM IDc mice through inhibition of osteoclastogenesis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1640282-42-3
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Appearance Solid
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Molecular Weight 513.92
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Formula C25H22ClF2N5O3
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Color White to yellow
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SMILES
FC1=CC(F)=CN=C1COC2=C(Cl)C(N(C3=CC(C4=NC(C(C)(C)O)=NC=C4)=NC=C3C)C(C)=C2)=O
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Synonyms
ATI-450; CDD-450
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (194.58 mM; Need ultrasonic; 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: ≥ 2.5 mg/mL (4.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Purity & Documentation
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Data Sheet (278 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
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 | 1.9458 mL | 9.7291 mL | 19.4583 mL | 48.6457 mL |
| 5 mM | 0.3892 mL | 1.9458 mL | 3.8917 mL | 9.7291 mL | |
| 10 mM | 0.1946 mL | 0.9729 mL | 1.9458 mL | 4.8646 mL | |
| 15 mM | 0.1297 mL | 0.6486 mL | 1.2972 mL | 3.2430 mL | |
| 20 mM | 0.0973 mL | 0.4865 mL | 0.9729 mL | 2.4323 mL | |
| 25 mM | 0.0778 mL | 0.3892 mL | 0.7783 mL | 1.9458 mL | |
| 30 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6215 mL | |
| 40 mM | 0.0486 mL | 0.2432 mL | 0.4865 mL | 1.2161 mL | |
| 50 mM | 0.0389 mL | 0.1946 mL | 0.3892 mL | 0.9729 mL | |
| 60 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8108 mL | |
| 80 mM | 0.0243 mL | 0.1216 mL | 0.2432 mL | 0.6081 mL | |
| 100 mM | 0.0195 mL | 0.0973 mL | 0.1946 mL | 0.4865 mL |
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