Evobrutinib
Based on 11 publication(s) in Google Scholar
Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTK inhibitor, with an IC50 of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.60%
- CAS No.: 1415823-73-2
- Formule: C25H27N5O2
- Masse moléculaire:429.51
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Anti-Infection Compound Library
HY-L002
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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Protein Tyrosine Kinase Compound Library
HY-L016
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Clinical Compound Library
HY-L026
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Drug Repurposing Compound Library
HY-L035
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Covalent Screening Library
HY-L036
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Anti-COVID-19 Compound Library
HY-L052
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Orally Active Compound Library
HY-L061
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Anti-Blood Cancer Compound Library
HY-L079
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Rare Diseases Drug Library
HY-L102
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Cysteine Targeted Covalent Library
HY-L153
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Autoimmune Disease Compound Library
HY-L156
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Highly Selective Inhibitors Library
HY-L158
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Anti-Hematopathy Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Covalent Screening Library Plus
HY-L036P
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Bioactive Compound Library
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Protein Kinase Compound Library
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Rheumatic Arthritis Compound Library
HY-L210
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Evobrutinib
More- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Eur J Pharmacol. 2022 Jan 5:914:174690. [Abstract]
- Thromb Haemost. 2019 Mar;119(3):397-406. [Abstract]
- iScience. 2024 Sep 24;27(11):110961. [Abstract]
- Sci Rep. 2026 Mar 20;16(1):14300. [Abstract]
- ACS Pharmacol Transl Sci. 2025 Mar 12;8(4):917-931. [Abstract]
- Drug Test Anal. 2019 Jan;11(1):129-139. [Abstract]
- Biomed Chromatogr. 2019 May;33(5):e4507. [Abstract]
- bioRxiv. 2026 Jun 8:2026.06.03.729882. [Abstract]
- bioRxiv. 2024 September 08.
- J Immunol Sci. March 31, 2022.
Activité biologique
IC50: 8.9 nM (BTK)[1]
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Cell Line
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Type | Value | Description | References |
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| PBMC | IC50 |
66.3 nM
Compound: Evobrutinib
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Antiinflammatory activity in human PBMC assessed as inhibition of anti-IgM induced CD69 expression incubated for 2 hrs followed by goat F(ab') 2 anti-human IgM addition measured after 18 hrs by flow cytometry analysis
Antiinflammatory activity in human PBMC assessed as inhibition of anti-IgM induced CD69 expression incubated for 2 hrs followed by goat F(ab') 2 anti-human IgM addition measured after 18 hrs by flow cytometry analysis
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[PMID: 36462441] |
| Sf21 | IC50 |
5800 nM
Compound: A18; M2951
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Inhibition of N-terminal GST-tagged human EGFR (696 to end aminoacids) expressed in baculovirus infected Sf21 cells
Inhibition of N-terminal GST-tagged human EGFR (696 to end aminoacids) expressed in baculovirus infected Sf21 cells
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[PMID: 31368705] |
| TMD8 | IC50 |
56.2 nM
Compound: Evobrutinib
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Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 35939993] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rats with semi-established type II collagen arthritis[1].
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Dosage:0.3, 1, 3, 10, or 30 mg/kg.
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Administration:Oral gavage once daily for 11 days (days 6-16).
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Result:Reduced ankle histopathology scores in a dose-dependent manner, compared to vehicle.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1415823-73-2
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Appearance Solid
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Masse moléculaire 429.51
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Formule C25H27N5O2
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Color White to off-white
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SMILES
C=CC(N1CCC(CNC2=NC=NC(N)=C2C3=CC=C(OC4=CC=CC=C4)C=C3)CC1)=O
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Synonyms
M2951; MSC2364447C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (11)
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Journal Impact Factor
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Most Recent
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Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Eur J Pharmacol
The immunomodulatory effect of koumine on B cells under dependent and independent responses by T cells. [Abstract]2022 Jan 5:914:174690. PMID: 34890543 -
Thromb Haemost
Optimizing Platelet GPVI Inhibition versus Haemostatic Impairment by the Btk Inhibitors Ibrutinib, Acalabrutinib, ONO/GS-4059, BGB-3111 and Evobrutinib. [Abstract]2019 Mar;119(3):397-406. PMID: 30685871 -
iScience
Inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746. [Abstract]2024 Sep 24;27(11):110961. PMID: 39759071 -
Sci Rep
2026 Mar 20;16(1):14300. PMID: 41862552 -
ACS Pharmacol Transl Sci
Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]2025 Mar 12;8(4):917-931. PMID: 40242575 -
Drug Test Anal
Identification of metabolites of evobrutinib in rat and human hepatocytes by using ultra-high performance liquid chromatography coupled with diode array detector and Q Exactive Orbitrap tandem mass spectrometry. [Abstract]2019 Jan;11(1):129-139. PMID: 30102849 -
Biomed Chromatogr
The effect of naringenin on the pharmacokinetics of ibrutinib in rat: A drug-drug interaction study. [Abstract]2019 May;33(5):e4507. PMID: 30754071 -
bioRxiv
Cross-presentation of citrullinated antigens drives cytotoxic CD8 + T cell responses in rheumatoid arthritis. [Abstract]2026 Jun 8:2026.06.03.729882. PMID: 42327047 -
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Solvant et solubilité
DMSO : 33.33 mg/mL (77.60 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: ≥ 2.08 mg/mL (4.84 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.84 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.3282 mL | 11.6412 mL | 23.2823 mL | 58.2059 mL |
| 5 mM | 0.4656 mL | 2.3282 mL | 4.6565 mL | 11.6412 mL | |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3282 mL | 5.8206 mL | |
| 15 mM | 0.1552 mL | 0.7761 mL | 1.5522 mL | 3.8804 mL | |
| 20 mM | 0.1164 mL | 0.5821 mL | 1.1641 mL | 2.9103 mL | |
| 25 mM | 0.0931 mL | 0.4656 mL | 0.9313 mL | 2.3282 mL | |
| 30 mM | 0.0776 mL | 0.3880 mL | 0.7761 mL | 1.9402 mL | |
| 40 mM | 0.0582 mL | 0.2910 mL | 0.5821 mL | 1.4551 mL | |
| 50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.1641 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9701 mL |
Evobrutinib Related Classifications
HY-101215 Related Classifications
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