1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. (±)-Zanubrutinib

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

Cat. No.: HY-101474 Purity: 99.73%
COA Handling Instructions

(±)-Zanubrutinib ((±)-BGB-3111) est un inhibiteur de tyrosine kinase de Bruton (Btk) qui est puissant, sélectif et oralement disponible.

(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.

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

(±)-Zanubrutinib Chemical Structure

(±)-Zanubrutinib Chemical Structure

CAS No. : 1633350-06-7

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
5 mg USD 140 In-stock
10 mg USD 220 In-stock
50 mg USD 660 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of (±)-Zanubrutinib:

Top Publications Citing Use of Products

    (±)-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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    (±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor[1].

    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.
    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
    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)

    Mass
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    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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: 99.73%

    References

    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.

    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
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    (±)-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.

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    Product Name:
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