Evobrutinib (M-2951): BTK Inhibitor FAQs & Research Guide
Evobrutinib (M-2951): BTK Inhibitor FAQs & Research Guide
Evobrutinib (M-2951) is a selective, covalent Bruton's tyrosine kinase (BTK) inhibitor investigated for its role in modulating B-cell and immune-cell signaling in autoimmune and oncological research settings.
- Product Name
- Evobrutinib (M-2951)
- SKU
- E421538
- Target
- Bruton's Tyrosine Kinase (BTK)
- Inhibitor Type
- Selective covalent (irreversible) BTK inhibitor
- Primary Research Areas
- Autoimmune disease, B-cell malignancies, immunology
- Reference SKU
- E414173
What Is Evobrutinib (M-2951) and How Does It Work?
Evobrutinib, also designated M-2951, is a small-molecule inhibitor that selectively and covalently targets Bruton's tyrosine kinase (BTK), a non-receptor tyrosine kinase critical to B-cell receptor (BCR) signaling. By forming an irreversible covalent bond with a cysteine residue (Cys481) in the BTK active site, Evobrutinib permanently suppresses kinase activity, thereby blocking downstream signaling pathways involved in B-cell proliferation, survival, and activation.
In research contexts, Evobrutinib serves as a valuable pharmacological tool for dissecting BTK-dependent pathways in immune cells, including B cells, mast cells, and macrophages. Its covalent mechanism of action provides sustained target engagement, which is advantageous in in vitro and in vivo experimental models.
Solubility, Storage, and Handling Recommendations
Proper handling of Evobrutinib (M-2951) is essential to maintain compound integrity and experimental reproducibility. As a general guideline for small-molecule kinase inhibitors of this class:
- Solubility: Evobrutinib is typically soluble in DMSO. It is recommended to prepare concentrated stock solutions in DMSO and dilute into aqueous buffers or cell culture media immediately before use. Final DMSO concentrations in assay systems should generally not exceed 0.1–0.5% to avoid cytotoxicity artifacts.
- Storage: Store the compound as a solid at –20°C or –80°C, protected from light and moisture. Avoid repeated freeze-thaw cycles of stock solutions.
- Handling: Work under standard laboratory safety precautions. Consult the Safety Data Sheet (SDS) before use.
Note: Specific solubility values and confirmed storage conditions for SKU E421538 should be verified against the Certificate of Analysis (CoA) and product datasheet available from Aladdin Scientific.
Research Applications of Evobrutinib (M-2951)
Evobrutinib has been employed across several key research domains:
- Autoimmune Disease Research: As a BTK inhibitor, Evobrutinib has been studied for its ability to suppress aberrant B-cell activation implicated in conditions such as multiple sclerosis (MS), rheumatoid arthritis (RA), and systemic lupus erythematosus (SLE).
- B-Cell Malignancy Models: BTK inhibition is a well-validated strategy in B-cell lymphomas and leukemias. Evobrutinib can be used in cell-line and primary-cell models to probe BTK-driven proliferative and survival signals.
- Mast Cell and FcR Signaling: BTK also plays a role downstream of Fc receptors in mast cells and basophils, making Evobrutinib relevant to allergy and innate immune research.
- Comparative BTK Inhibitor Studies: Researchers may use Evobrutinib alongside other BTK inhibitors to compare selectivity profiles and assess off-target effects in signaling pathway analyses.
Frequently asked questions
What is the molecular target of Evobrutinib (M-2951)?
Evobrutinib (M-2951) selectively targets Bruton's tyrosine kinase (BTK). It acts as a covalent, irreversible inhibitor by binding to the Cys481 residue within the BTK active site, thereby blocking BTK-mediated downstream signaling in B cells and other immune cell types.
In what solvent is Evobrutinib (M-2951) typically dissolved for in vitro assays?
Evobrutinib is generally dissolved in DMSO to prepare stock solutions for in vitro use. The stock is then diluted into the appropriate aqueous medium immediately before the experiment. Researchers should verify specific solubility data in the product CoA and keep final DMSO concentrations within levels tolerated by the cell system under study.
What are the primary research applications for Evobrutinib (M-2951)?
Evobrutinib is primarily used as a pharmacological tool compound to study BTK-dependent signaling in immunology and oncology research contexts. Key applications include investigating B-cell receptor signaling, modeling autoimmune conditions such as multiple sclerosis and rheumatoid arthritis, and examining BTK's role in B-cell malignancies and Fc receptor-mediated immune responses.
How should Evobrutinib (M-2951) be stored to maintain stability?
As a general best practice for covalent small-molecule inhibitors, Evobrutinib should be stored as a solid at –20°C or –80°C in a dry, light-protected environment. Prepared DMSO stock solutions should be aliquoted to minimize freeze-thaw cycles. Always refer to the specific storage conditions stated on the product datasheet and CoA supplied by Aladdin Scientific.
What is the difference between SKU E421538 and the referenced SKU E414173?
The source material indicates that SKU E421538 (Evobrutinib, M-2951) references SKU E414173. The precise differences in formulation, purity grade, or pack size between these two entries have not been specified in the available documentation. Researchers should consult the individual product datasheets or contact Aladdin Scientific customer service for clarification before ordering.
References
- Evobrutinib (M-2951) product page, Aladdin Scientific, SKU E421538.
- Reference product E414173, Aladdin Scientific — relationship to E421538 requires clarification.
- BTK as a therapeutic target in B-cell-driven autoimmune diseases — general literature. Specific publications not provided in source material.
Products are supplied for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
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