Name: Zanubrutinib (BGB-3111)
Brand: Selleck Chemicals
SKU: S8791
Availability: InStock
Rating: 5 (3 reviews)

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Quality Control

Batch: Purity: 99.79%

99.79

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other BTK Inhibitors	Spebrutinib (AVL-292) tirabrutinib(ONO-4059) hydrochloride CGI1746 LFM-A13 CNX-774 BMS-935177 Fenebrutinib (GDC-0853) Branebrutinib (BMS-986195) Evobrutinib BMS-986142

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

+

%

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

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 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06029309	Not yet recruiting	Mantle Cell Lymphoma	Alvaro Alencar MD\|BeiGene\|Incyte Corporation\|MorphoSys AG\|University of Miami	May 1 2024	Phase 1\|Phase 2
NCT06350318	Recruiting	Follicular Lymphoma\|Marginal Zone Lymphoma\|B-Cell Lymphoma	H. Lee Moffitt Cancer Center and Research Institute\|BeiGene Ltd.	March 13 2024	Phase 2
NCT06067048	Not yet recruiting	Lymphoma	Stichting Hemato-Oncologie voor Volwassenen Nederland	February 1 2024	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

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Handling Instructions

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Zanubrutinib (BGB-3111) BTK inhibitor

Chemical Structure

Molecular Weight: 471.55