| Name | (±)-Zanubrutinib |
| Description | (±)-Zanubrutinib ((±)-BGB-3111) is a potent, orally available Bruton's tyrosine kinase (Btk) inhibitor, exhibiting superior oral bioavailability, higher exposure, and more complete target inhibition. |
| In vitro | In both biochemical and cellular assays, (±)-Zanubrutinib exhibits nanomolar Btk inhibition activity. Compared to ibrutinib, (±)-Zanubrutinib shows significantly more restricted off-target activities against a panel of kinases, including ITK. In various MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and effectively inhibits cell proliferation[1]. |
| In vivo | (±)-Zanubrutinib exhibits dose-dependent anti-tumor properties in mice with REC-1 MCL xenografts, regardless of whether the xenografts are engrafted subcutaneously or through systemic injection via the tail vein. A preliminary 14-day toxicity study in rats indicates that (±)-Zanubrutinib is exceptionally well-tolerated, with a maximally tolerated dose (MTD) remaining undetermined at dosages up to 250mg/kg/day[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (106.03 mM)
Ethanol : 9.0 mg/mL (19.1 mM)
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| Keywords | BGB-3111 | Zanubrutinib | BGB 3111 | BGB3111 |
| Inhibitors Related | CP-547632 | Ibrutinib | IBT6A | Orelabrutinib |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Covalent Inhibitor Library |
United States
