Cat. No.: HY-101474A

Zanubrutinib

(Synonyms: BGB-3111)

24 Cited Publications

Customer Review

Based on 24 publication(s) in Google Scholar

Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC₅₀: 0.3 nM).

For research use only. We do not sell to patients.

Purity: 99.71%
CAS No.: 1691249-45-2
Formula: C₂₇H₂₉N₅O₃
Molecular Weight:471.55

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Zanubrutinib Chemical Structure

CAS No.: 1691249-45-2

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC₅₀: 0.3 nM)^[1]^[2].

IC₅₀ & Target

BTK^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	204.7 nM Compound: 31a; BGB-3111	Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay	[PMID: 31381333]
HEK-293T	IC₅₀	39136 nM Compound: Zanubrutinib	Antiproliferative activity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34391034]
Jurkat	IC₅₀	3477 nM Compound: 31a; BGB-3111	Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis	[PMID: 31381333]
MOLM-13	IC₅₀	5095 nM Compound: Zanubrutinib	Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34391034]
OCI-Ly10	IC₅₀	0.35 nM Compound: 31a; BGB-3111	Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay	[PMID: 31381333]
Ramos	IC₅₀	1.8 nM Compound: 31a; BGB-3111	Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay	[PMID: 31381333]
Ramos	IC₅₀	>30000 nM Compound: Zanubrutinib	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34391034]
Rec1	IC₅₀	0.36 nM Compound: 31a; BGB-3111	Antiproliferative activity against human Rec1 cells after 6 days by Celltiter-glo luminescent cell viability assay Antiproliferative activity against human Rec1 cells after 6 days by Celltiter-glo luminescent cell viability assay	[PMID: 31381333]
Rec1	IC₅₀	0.36 nM Compound: (S)-3	Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay	[PMID: 36912866]
Sf9	IC₅₀	0.3 nM Compound: 31a; BGB-3111	Inhibition of N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FR Inhibition of N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FR	[PMID: 31381333]
TMD8	IC₅₀	3.8 nM Compound: Zanubrutinib	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34391034]

In Vitro

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor. In both biochemical and cellular assays, Zanubrutinib demonstrates nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, Zanubrutinib inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with PCI-32765, Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Zanubrutinib (BGB-3111) induces 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 shows similar activity as PCI-32765 at 50 mg/kg QD. In the systemic model, the median survival of Zanubrutinib 25 mg/kg BID group is significantly longer than those of both PCI-32765 50 mg/kg QD and BID groups. In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, Zanubrutinib also demonstrates better anti-tumor activity than PCI-32765. Preliminary 14-day toxicity study in rats shows that Zanubrutinib is very well tolerated and maximal tolerate dose (MTD) is not reached when it is dosed up to 250 mg/kg/day^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1691249-45-2
Appearance Solid
Molecular Weight 471.55
Formula C₂₇H₂₉N₅O₃
Color White to off-white
SMILES

NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)[C@H](C5CCN(C(C=C)=O)CC5)CCN2)=O
Synonyms

BGB-3111
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (24)

All Flow CytometryCell Proliferation/Viability AssayRT-PCR

Sort by:

Journal Impact Factor

Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Blood Adv

Zanubrutinib and pirtobrutinib show synergistic killing and suppression of BTK signaling in MYD88-mutated lymphoma cells. [Abstract]

2026 Jul 14;10(13):4450-4454. PMID: 41985014
Blood Adv

PLCG2 Exon-Skipped Variants: Insights into Their Potential Role in Chronic Lymphocytic Leukemia. [Abstract]

2026 Jun 5:bloodadvances.2025019077. PMID: 42263669
J Med Chem

Discovery of 1-Amino-1 H-imidazole-5-carboxamide Derivatives as Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitors. [Abstract]

2021 Nov 11;64(21):16242-16270. PMID: 34672559
Antioxidants (Basel)

Genome-Wide RNAi Screening Identifies Novel Pathways/Genes Involved in Oxidative Stress and Repurposable Drugs to Preserve Cystic Fibrosis Airway Epithelial Cell Integrity. [Abstract]

2021 Dec 2;10(12):1936. PMID: 34943039
Pharmaceutics

Design and Characterization of a Novel Venetoclax-Zanubrutinib Nano-Combination for Enhancing Leukemic Cell Uptake and Long-Acting Plasma Exposure. [Abstract]

2023 Mar 22;15(3):1016. PMID: 36986876
Pharmaceutics

Bruton's Tyrosine Kinase Inhibitor Zanubrutinib Effectively Modulates Cancer Resistance by Inhibiting Anthracycline Metabolism and Efflux. [Abstract]

2022 Sep 21;14(10):1994. PMID: 36297430

Zanubrutinib purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2022 Sep 21;14(10):1994. [Abstract]

Flow cytometry analysis of daunorubicin (DAUN) accumulation in A549 and KG1α cells. A549 and KG1α cells were preincubated with Zanubrutinib (ZAN) (1, 5, 10, and 25 µM) were added to the cells.

Zanubrutinib purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2022 Sep 21;14(10):1994. [Abstract]

HepG2 and KG1α cells were treated with Zanubrutinib (ZAN) (0.1–50 µM) or dimethyl sulfoxide (DMSO) (a vehicle) for 48 h, and the cell viability was evaluated by the XTT test.

Zanubrutinib purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2022 Sep 21;14(10):1994. [Abstract]

qRT-PCR was used to monitor changes in AKR1C3 mRNA expression following a 24 and 48 h incubation with Zanubrutinib (ZAN) (0.5 μM).
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Thromb Haemost

Optimizing Platelet GPVI Inhibition versus Haemostatic Impairment by the Btk Inhibitors Ibrutinib, Acalabrutinib, ONO/GS-4059, BGB-3111 and Evobrutinib. [Abstract]

2019 Mar;119(3):397-406. PMID: 30685871
iScience

Inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746. [Abstract]

2024 Sep 24;27(11):110961. PMID: 39759071
Sci Rep

Cysteine-reactive mitigators of small vessel disease-related NOTCH3 mutants. [Abstract]

2026 Mar 20;16(1):14300. PMID: 41862552
Anal Bioanal Chem

Development, validation, and clinical application of LC-MS/MS method for simultaneous determination of ibrutinib, zanubrutinib, orelabrutinib, acalabrutinib, and their active metabolites in patients with B-cell lymphoma. [Abstract]

2025 Feb;417(4):821-834. PMID: 39702674
ACS Pharmacol Transl Sci

Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]

2025 Mar 12;8(4):917-931. PMID: 40242575
PLoS One

Investigation of the anti-tumor mechanism of tirabrutinib, a highly selective Bruton's tyrosine kinase inhibitor, by phosphoproteomics and transcriptomics. [Abstract]

2023 Mar 10;18(3):e0282166. PMID: 36897912
Acta Chromatogr

2025 Jan 07.
Hematology

Brutons tyrosine kinase inhibitor Zanubrutinib modulates Fc gamma receptors to inhibit platelet destruction for alleviation of refractory immune thrombocytopenia. [Abstract]

2025 Dec;30(1):2545078. PMID: 41047944
bioRxiv

More than an attachment module: covalent inhibitor warheads influence BTK dynamics and function. [Abstract]

2026 May 8:2026.05.07.723540. PMID: 42146433
bioRxiv

2024 September 08.
SSRN

2024 Mar 6.
bioRxiv

Impact of the clinically approved BTK inhibitors on the conformation of full-length BTK and analysis of the development of BTK resistance mutations in chronic lymphocytic leukemia. [Abstract]

2024 Oct 10:2023.12.18.572223. PMID: 38187560
Preprints

2023 Jun 19.
Patent

US20230113802A1.
bioRxiv

2023 Feb 24.
Ludwig Maximilian University of Munich

2021 May.

Solvent & Solubility

In Vitro:

DMSO : 175 mg/mL (371.12 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1207 mL

10.6033 mL

21.2067 mL

5 mM

0.4241 mL

2.1207 mL

4.2413 mL

10 mM

0.2121 mL

1.0603 mL

2.1207 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Na Li, et al. Abstract 2597: BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. Cancer Res 2015;75(15 Suppl):Abstract nr 2597.

[2]. Guo Y, et al. Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. J Med Chem. 2019 Sep 12;62(17):7923-7940. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1207 mL	10.6033 mL	21.2067 mL	53.0166 mL
	5 mM	0.4241 mL	2.1207 mL	4.2413 mL	10.6033 mL
	10 mM	0.2121 mL	1.0603 mL	2.1207 mL	5.3017 mL
	15 mM	0.1414 mL	0.7069 mL	1.4138 mL	3.5344 mL
	20 mM	0.1060 mL	0.5302 mL	1.0603 mL	2.6508 mL
	25 mM	0.0848 mL	0.4241 mL	0.8483 mL	2.1207 mL
	30 mM	0.0707 mL	0.3534 mL	0.7069 mL	1.7672 mL
	40 mM	0.0530 mL	0.2651 mL	0.5302 mL	1.3254 mL
	50 mM	0.0424 mL	0.2121 mL	0.4241 mL	1.0603 mL
	60 mM	0.0353 mL	0.1767 mL	0.3534 mL	0.8836 mL
	80 mM	0.0265 mL	0.1325 mL	0.2651 mL	0.6627 mL
	100 mM	0.0212 mL	0.1060 mL	0.2121 mL	0.5302 mL

Keywords

Zanubrutinib

24 Cited Publications

100 mg Get Quote

Subscribe to the

MedChemExpress

Newsletter

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Zanubrutinib

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Blood Cancer Compound Library

Targeted Therapy Drug Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Non-steroidal Anti-Inflammatory Compound Library

Heterocyclic Compound Library

Cysteine Targeted Covalent Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Zanubrutinib

Biological Activity

Chemical Information

Publications (24)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Zanubrutinib Related Classifications

HY-101474A Related Classifications