Zanubrutinib (BGB-3111) is a potent, selective, and orally active covalent inhibitor of Bruton's tyrosine kinase (BTK), with an IC50 of 0.3 nM. It shows high selectivity for BTK over a panel of 304 kinases at 1?μM, although it also inhibits EGFR, Tec, Blk, BMX, HER4, and TXK (IC50s ranging from 0.62 to 33 nM). Zanubrutinib blocks BTK phosphorylation at Y223 (IC50 = 1.8 nM) in Ramos cells and reduces REC-1 cell viability (IC50 = 0.36 nM). In vivo, it decreases tumor volume in OCI-LY10 DLBCL xenograft models at doses of 2.5 and 7.5 mg/kg.
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