(±)-Zanubrutinib is a specific, potent and orally available Btk inhibitor.

In both biochemical and cellular assays, (±)-Zanubrutinib demonstrates nanomolar Btk inhibition activity. In comparison with ibrutinib, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK. In several MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation.

(±)-Zanubrutinib induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice. In the subcutaneous xenografts. Preliminary 14-day toxicity study in rats shows that (±)-Zanubrutinib is a very well tolerated and maximally tolerated dose (MTD) is not reached when it is dosed up to 250mg/kg/day.

1633350-06-7

C27H29N5O3

471.55

(±)-BGB-3111;(±)-赞鲁替尼

DMSO:28 mg/mL (59.38 mM)
Ethanol:10 mg/mL (21.21 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years