Home Protein Tyrosine Kinase BTK inhibitor Zanubrutinib For research use only.

Zanubrutinib

Synonyms: BGB-3111

Zanubrutinib 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 Chemical Structure

Zanubrutinib Chemical Structure

CAS: 1691249-45-2

Selleck's Zanubrutinib has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.69%
99.69

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Biological Activity

Description Zanubrutinib 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 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].
Experimental Result Images Methods Biomarkers Images PMID
Western blot BTK / IRF4 / p-BTK-Tyr223 p-STAT3 / STAT3 / NFATc1 / PD-L1 30679329
ELISA IL-10 30209121
In Vivo
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06067048 Not yet recruiting Lymphoma Stichting Hemato-Oncologie voor Volwassenen Nederland February 1 2024 Phase 2
NCT06029309 Not yet recruiting Mantle Cell Lymphoma Alvaro Alencar MD|BeiGene|Incyte Corporation|MorphoSys AG|University of Miami January 31 2024 Phase 1|Phase 2
NCT05665530 Recruiting Aggressive B-Cell Non-Hodgkin''s Lymphoma|Aggressive B-Cell NHL|Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma|Mantle Cell Lymphoma (MCL)|Richter''s Syndrome|T-cell Lymphoma Prelude Therapeutics|BeiGene September 12 2023 Phase 1
NCT05356858 Recruiting Neuromyelitis Optica Xuanwu Hospital Beijing May 7 2022 Phase 2

Chemical lnformation & Solubility

Molecular Weight 471.55 Formula

C27H29N5O3
CAS No. 1691249-45-2 SDF --
Smiles C=CC(=O)N1CCC(CC1)C2CCNC3=C(C(=NN23)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=O)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 94 mg/mL ( (199.34 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble


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In vivo
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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.

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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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