Zanubrutinib (BGB-3111)

Catalog No.S8791

For research use only.

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.

Zanubrutinib (BGB-3111) Chemical Structure

CAS No. 1691249-45-2

Purity & Quality Control

Choose Selective BTK Inhibitors

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.
Targets
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].

Assay
Methods Test Index PMID
Western blot BTK / IRF4 / p-BTK-Tyr223 ; p-STAT3 / STAT3 / NFATc1 / PD-L1 30679329 30209121
ELISA IL-10 30209121
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].

Protocol (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 471.55
Formula

C27H29N5O3

CAS No. 1691249-45-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C=CC(=O)N1CCC(CC1)C2CCNC3=C(C(=NN23)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04643470 Recruiting Drug: Zanubrutinib|Drug: Placebo Lupus Nephritis BeiGene December 22 2020 Phase 2
NCT04470908 Completed Drug: Zanubrutinib|Drug: Rifabutin Healthy|Male BeiGene August 24 2020 Phase 1
NCT04458610 Recruiting Biological: Rituximab|Drug: Zanubrutinib Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) May 26 2020 Phase 2
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 25 2020 Phase 1|Phase 2
NCT04277637 Recruiting Drug: BGB-11417|Drug: Zanubrutinib Mature B-Cell Malignancies BeiGene March 24 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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