Name: Zanubrutinib (BGB-3111)
Brand: Selleck Chemicals
SKU: S8791
Availability: InStock
Rating: 5 (7 reviews)

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Quality Control

Batch: Purity: 99.79%

99.79

Related Targets	EGFR VEGFR FGFR PDGFR c-Met Src MEK CSF-1R FLT3 HER2
Other BTK Inhibitors	Catadegbrutinib (BGB-16673) Spebrutinib (AVL-292) tirabrutinib(ONO-4059) hydrochloride LFM-A13 CGI1746 Evobrutinib BMS-935177 CNX-774 Branebrutinib (BMS-986195) Fenebrutinib (GDC-0853)

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (199.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.700mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 94 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	471.55	Formula	C₂₇H₂₉N₅O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1691249-45-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BGB-3111			SMILES	C=CC(=O)N1CCC(CC1)C2CCNC3=C(C(=NN23)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=O)N

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	BTK (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. 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.
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. 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. 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.
References	[1] http://www.bloodjournal.org/content/126/23/832?sso-checked=true [2] http://cancerres.aacrjournals.org/content/75/15_Supplement/2597 [3] https://pubmed.ncbi.nlm.nih.gov/27590878/ [4] https://pubmed.ncbi.nlm.nih.gov/31381333/

Applications

Methods	Biomarkers	Images	PMID
Western blot	BTK / IRF4 / p-BTK-Tyr223 p-STAT3 / STAT3 / NFATc1 / PD-L1		30679329
ELISA	IL-10		30209121

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-02)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05976763	RECRUITING	Mantle Cell Lymphoma	Alliance for Clinical Trials in Oncology	2023-10-20	PHASE3
NCT07474961	NOT_YET_RECRUITING	Waldenstrom Macroglobulinaemia; Multiple Myeloma	Anne Louise Tølbøll Sørensen	2027-03	PHASE4
NCT07638722	NOT_YET_RECRUITING	Recurrent Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue; Recurrent Nodal Marginal Zone Lymphoma; Recurrent Splenic Marginal Zone Lymphoma; Refractory Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue; Refractory Nodal Marginal Zone Lymphoma; Refractory Splenic Marginal Zone Lymphoma	SWOG Cancer Research Network	2026-10-03	PHASE2
NCT06544785	RECRUITING	Chronic Lymphocytic Leukemia; Small Lymphocytic Lymphoma	PETHEMA Foundation	2024-09-02	PHASE2
NCT06073821	ACTIVE_NOT_RECRUITING	CLL	BeOne Medicines	2023-11-11	PHASE3
NCT06824701	ACTIVE_NOT_RECRUITING	Relapsed or Refractory B-cell Non-Hodgkin Lymphoma	University of Utah	2025-09-12	PHASE1

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Zanubrutinib (BGB-3111) BTK inhibitor

Chemical Structure

Molecular Weight: 471.55