Zanubrutinib (BGB-3111)

For research use only.

Catalog No.S8791

Zanubrutinib (BGB-3111) Chemical Structure

Molecular Weight(MW): 471.55

Zanubrutinib (BGB-3111) is a potent, specific and irreversible BTK inhibitor that has been shown to have a lower off-target inhibitory activity on other kinases, including ITK, JAK3 and EGFR.

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Biological Activity

Description Zanubrutinib (BGB-3111) is a potent, specific and irreversible BTK inhibitor that has been shown to have a lower off-target inhibitory activity on other kinases, including ITK, JAK3 and EGFR.
BTK [1]
(Cell-free assay)
In vitro

In biochemical and cellular assays, BGB-3111 is more selective than ibrutinib for BTK vs. EGFR, FGR, FRK, HER2, HER4, ITK, JAK3, LCK, BLK and TEC[1]. In several MCL and DLBCL cell lines, BGB-3111 inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation[2].

Methods Test Index PMID
Western blot
BTK / IRF4 / p-BTK-Tyr223 ; 

PubMed: 30679329     

Assessment of IRF4 and pBTK levels in mantle cell lymphoma cell lines exposed to first- and second-generation Bruton tyrosine kinase inhibitors. The REC1 and Jeko1 cell lines were exposed to ibrutinib (500 nM), zanubrutinib (500 nM), spebrutinib (500 nM), and dimethylsulfoxide (DMSO) for 24 h.

p-STAT3 / STAT3 / NFATc1 / PD-L1 ; 

PubMed: 30209121     

OCI-LY10 cells were treated with different doses of ibrutinib, APC-196, or BGB-3111 for 24 hours. Purified nuclear extracts were used to examine pSTAT3, STAT3, NFATc1, and lamin B (loading control) protein expression levels by western blotting. Cytoplasmic extracts were used to examine PD-L1 and actin (loading control). 

30679329 30209121

PubMed: 30209121     

OCI-LY10 and HBL-1 cells were treated with different BTK inhibitors (ibrutinib, ACP-196, and BGB-3111) at different doses for 24 hours. Supernatants collected from these samples were used to analyze IL-10 secretion using ELISA.

In vivo

In preclinical animal studies, BGB-3111 demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibition in the tissues than ibrutinib[1]. In mouse BTK occupancy assays, treatment with BGB-3111 results in a dose-dependent BTK occupancy and shows about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen[2]. Both in the REC-1 MCL and ABC subtype DLBCL (TMD-8) xenograft models, BGB-3111 induces dose-dependent anti-tumor effects and demonstrates superior efficacy in comparison with ibrutinib. Toxicity study in rats indicates that BGB-3111 is very well tolerated, and the MTD is not reached when it is dosed up to 250 mg/kg/day[3].


Solubility (25°C)

In vitro DMSO 94 mg/mL (199.34 mM)
Ethanol 94 mg/mL (199.34 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 471.55


CAS No. 1691249-45-2
Storage powder
in solvent
Synonyms N/A
Smiles NC(=O)C1=C2NCCC(C3CCN(CC3)C(=O)C=C)[N]2N=C1C4=CC=C(OC5=CC=CC=C5)C=C4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04282018 Recruiting Drug: BGB-10188|Drug: Zanubrutinib|Drug: Tislelizumab Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Follicular Lymphoma|Marginal Zone Lymphoma|Mantle Cell Lymphoma|Diffuse Large B Cell Lymphoma|Advanced Solid Tumor|Non-small Cell Lung Cancer|Metastatic Melanoma BeiGene May 2020 Phase 1|Phase 2
NCT04172246 Recruiting Drug: Zanubrutinib Mature B-cell Malignancies BeiGene January 29 2020 Phase 1|Phase 2
NCT03561298 Completed Drug: BGB-3111 and Drug Cocktail Healthy Subjects BeiGene June 7 2018 Phase 1
NCT03465059 Completed Drug: Zanubrutinib Hepatic Insufficiency & Healthy Subjects BeiGene May 30 2018 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID