Zanubrutinib (Synonyms: BGB-3111)

Name: Zanubrutinib
Brand: MedChemExpress
SKU: HY-101474A
Rating: 5.0 (21 reviews)

Cat. No.: HY-101474A Purity: 99.71%: Data Sheet
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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.

CAS No. : 1691249-45-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Based on 21 publication(s) in Google Scholar

Other Forms of Zanubrutinib:

21 Publications Citing Use of MCE Zanubrutinib

Flow Cytometry

Cell Proliferation/Viability Assay

RT-PCR

: Zanubrutinib purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2022 Sep 21;14(10):1994.; 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.; 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.; qRT-PCR was used to monitor changes in AKR1C3 mRNA expression following a 24 and 48 h incubation with Zanubrutinib (ZAN) (0.5 μM).

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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
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]
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]
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: (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]
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]
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-FRET assay 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-FRET assay	[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

Molecular Weight

471.55

Formula

C₂₇H₂₉N₅O₃

CAS No.

1691249-45-2

Appearance

Solid

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.71%

Select Batch:

Data Sheet (278 KB) SDS (644 KB)

COA (254 KB) HNMR (298 KB) RP-HPLC (243 KB) LCMS (93 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]

Complete Stock Solution Preparation Table

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

Zanubrutinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zanubrutinib1691249-45-2BGB-3111BGB3111BGB 3111BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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Zanubrutinib (Synonyms: BGB-3111)

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Other Forms of Zanubrutinib:

Zanubrutinib Related Antibodies

21 Publications Citing Use of MCE Zanubrutinib

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Purity & Documentation

References

Customer Review

Zanubrutinib Related Antibodies

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Complete Stock Solution Preparation Table

Zanubrutinib Related Classifications

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