(±)-Zanubrutinib (Synonyms: (±)-BGB-3111)

Name: (±)-Zanubrutinib
Brand: MedChemExpress
SKU: HY-101474
Rating: 5.0 (5 reviews)

Cat. No.: HY-101474 Purity: 99.41%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

(±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC₅₀ of 0.63 nM.

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

(±)-Zanubrutinib Chemical Structure

CAS No. : 1633350-06-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of (±)-Zanubrutinib:

Zanubrutinib In-stock
(R)-Zanubrutinib In-stock
Zanubrutinib-d₅ Get quote

3 Publications Citing Use of MCE (±)-Zanubrutinib

Proliferation Assay

: (±)-Zanubrutinib purchased from MedChemExpress. Usage Cited in: Dr. Wang from Chinese Academy of Sciences.; Determining IC₅₀ for Zanubrutinib. IC₅₀ values for Zanubrutinib are determined using the ADP-Glo^™ Kinase Assay. Curve fitting is performed using GraphPad Prism sigmoidal dose-response (variable slope) software.

: (±)-Zanubrutinib purchased from MedChemExpress. Usage Cited in: Dr. Wang from Chinese Academy of Sciences.; Determining IC₅₀ for Zanubrutinib. IC₅₀ values for Zanubrutinib are determined using the ADP-Glo^™ Kinase Assay. Curve fitting is performed using GraphPad Prism sigmoidal dose-response (variable slope) software.

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References
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Description

(±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC₅₀ of 0.63 nM^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.63 nM Compound: 31	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]

In Vitro

In both biochemical and cellular assays, (±)-Zanubrutinib ((±)-BGB-3111) 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 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. 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 250mg/kg/day^[1].

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

Molecular Weight

471.55

Formula

C₂₇H₂₉N₅O₃

CAS No.

1633350-06-7

Appearance

Solid

Color

White to light yellow

SMILES

NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)C(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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL (63.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 10 mg/mL (21.21 mM)

*"≥" means soluble, but saturation unknown.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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: 99.70%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (254 KB) HNMR (233 KB) LCMS (360 KB)

Handling Instructions (2659 KB)

References

[1]. Na L, et al. BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Ethanol / 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
DMSO	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

(±)-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:

(±)-Zanubrutinib1633350-06-7(±)-BGB-3111BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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(±)-Zanubrutinib (Synonyms: (±)-BGB-3111)

Customer Review

Other Forms of (±)-Zanubrutinib:

(±)-Zanubrutinib Related Antibodies

3 Publications Citing Use of MCE (±)-Zanubrutinib

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Biological Activity

Purity & Documentation

References

Customer Review

(±)-Zanubrutinib Related Antibodies

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Complete Stock Solution Preparation Table

(±)-Zanubrutinib Related Classifications

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