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zanubrutinib

Name: zanubrutinib
Brand: TargetMol
SKU: T7584
Price: 54 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7584Cas No. 1691249-45-2

Alias BGB-3111

Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).

zanubrutinib

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Purity: 99.76%

Catalog No. T7584Alias BGB-3111Cas No. 1691249-45-2

Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$54	In Stock	In Stock
2 mg	$81	In Stock	In Stock
5 mg	$140	In Stock	In Stock
10 mg	$250	In Stock	In Stock
25 mg	$519	In Stock	In Stock
50 mg	$777	In Stock	In Stock
100 mg	$1,070	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$145	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.76%

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).
Targets&IC50	OCI-LY1 cells:0.35 nM, Sf9 cells:0.3 nM, TMD8 cells:3.8 nM, Ramos cells:1.8 nM, Jurkat cells:3477 nM, MOLM-13 cells:5095 nM, BTK:0.3 nM, Rec1 cells:0.36 nM, HEK293 cells:204.7 nM
In vitro	In both biochemical and cellular assays, zanubrutinib demonstrated nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, zanubrutinib inhibited BCR aggregation-triggered BTK autophosphorylation, blocked downstream PLC-γ2 signaling, and potently inhibited cell proliferation. In comparison with ibrutinib, zanubrutinib showed much more restricted off-target activities against a panel of kinases, including ITK. While ibrutinib significantly inhibited rituximab-induced NK cell IFN-γ secretion and in vitro cytotoxicity on mantle cell lymphoma cells, zanubrutinib was at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity[1].
In vivo	In mouse BTK occupancy assays, treatment with zanubrutinib resulted in a dose-dependent BTK occupancy and showed about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen.zanubrutinib induced 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 showed similar activity as ibrutinib at 50 mg/kg QD, its clinical relevant dose.In the systemic model, the median survival of zanubrutinib 25 mg/kg BID group was significantly longer than those of both ibrutinib 50 mg/kg QD and BID groups.In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, zanubrutinib also demonstrated better anti-tumor activity than ibrutinib.Preliminary 14-day toxicity study in rats showed that zanubrutinib was very well tolerated and maximal tolerate dose (MTD) was not reached when it was dosed up to 250mg/kg/day[1].
Synonyms	BGB-3111

Chemical Properties

Molecular Weight	471.55
Formula	C₂₇H₂₉N₅O₃
Cas No.	1691249-45-2
Smiles	NC(=O)c1c2NCC[C@@H](C3CCN(CC3)C(=O)C=C)n2nc1-c1ccc(Oc2ccccc2)cc1
Relative Density.	1.33 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 257.5 mg/mL (546.07 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.6 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1207 mL	10.6033 mL	21.2067 mL	106.0333 mL
5 mM	0.4241 mL	2.1207 mL	4.2413 mL	21.2067 mL
10 mM	0.2121 mL	1.0603 mL	2.1207 mL	10.6033 mL
20 mM	0.1060 mL	0.5302 mL	1.0603 mL	5.3017 mL
50 mM	0.0424 mL	0.2121 mL	0.4241 mL	2.1207 mL
100 mM	0.0212 mL	0.1060 mL	0.2121 mL	1.0603 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc