Tirabrutinib HCl

Tirabrutinib HCl (CAS No.: 1439901-97-9) is a synthetic small-molecule, highly selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor, commonly used in laboratory research in immunology and tumor biology, and is especially suitable for elucidating the dependence of B cell receptor (BCR) pathways and the regulatory mechanisms of kinase signaling networks; through covalent binding to BTK, it continuously inhibits BCR-driven signal transduction in B cell lines, and can lead to reduced downstream pathway readouts such as PLCγ2、NF?κB、AKT and ERK, decreased intracellular calcium flux, and restricted B cell activation and proliferation; in in vitro enzymatic and cellular assays, it typically exhibits nanomolar-level inhibitory activity, and shows significant selectivity separation from Src family members (such as LCK、LYN、Fyn), with selectivity ranges often extending to the micromolar level; in multiple preclinical systems (including B cell malignancy cell models such as TMD8 and corresponding mouse xenograft experiments), it can be used as a research tool to evaluate signaling pathway inhibition and tumor-related biological effects, and has shown a certain capacity for brain tissue exposure in animal studies, thereby supporting the investigation of peripheral and central BTK biology; typical applications include target occupancy and binding validation, phosphorylation signaling analysis, cell survival and apoptosis assessment, and efficacy or pharmacodynamic studies in mouse models; the concentration or dose used in specific experiments should be optimized according to the experimental design and research objectives; this product is for research use only and is prohibited for human or veterinary applications.