| Name | zanubrutinib |
| Description | Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK). |
| In vitro | In both biochemical and cellular assays, zanubrutinib demonstrated nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, zanubrutinib inhibited BCR aggregation-triggered BTK autophosphorylation, blocked downstream PLC-γ2 signaling, and potently inhibited cell proliferation. In comparison with ibrutinib, zanubrutinib showed much more restricted off-target activities against a panel of kinases, including ITK. While ibrutinib significantly inhibited rituximab-induced NK cell IFN-γ secretion and in vitro cytotoxicity on mantle cell lymphoma cells, zanubrutinib was at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity[1]. |
| In vivo | In mouse BTK occupancy assays, treatment with zanubrutinib resulted in a dose-dependent BTK occupancy and showed about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen.zanubrutinib induced 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, zanubrutinib at 2.5 mg/kg BID showed similar activity as ibrutinib at 50 mg/kg QD, its clinical relevant dose.In the systemic model, the median survival of zanubrutinib 25 mg/kg BID group was significantly longer than those of both ibrutinib 50 mg/kg QD and BID groups.In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, zanubrutinib also demonstrated better anti-tumor activity than ibrutinib.Preliminary 14-day toxicity study in rats showed that zanubrutinib was very well tolerated and maximal tolerate dose (MTD) was not reached when it was dosed 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 : 65 mg/mL (137.84 mM), Sonication is recommended.
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| Keywords | Btk | zanubrutinib | BGB3111 | Inhibitor | BGB 3111 | inhibit | Bruton tyrosine kinase |
| Inhibitors Related | evobrutinib | (±)-Zanubrutinib | CP-547632 | BMS-986142 | Edralbrutinib | Ibrutinib | IBT6A | Orelabrutinib | Atuzabrutinib | CGI-1746 |
| Related Compound Libraries | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
