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.
Usually ships within 24 hours.