1. Protein Tyrosine Kinase/RTK
  2. Btk

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

Cat. No.: HY-101474 Purity: 99.70%
Handling Instructions

(±)-Zanubrutinib 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
10 mM * 1 mL in DMSO USD 145 In-stock
1 mg USD 90 In-stock
5 mg USD 140 In-stock
10 mg USD 220 In-stock
50 mg USD 880 In-stock
100 mg USD 1400 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of (±)-Zanubrutinib:

    (±)-Zanubrutinib purchased from MCE. 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 MCE. 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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    In Vitro

    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 ibrutinib, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK. (±)-Zanubrutinib is at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity[1].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    471.55

    Formula

    C₂₇H₂₉N₅O₃

    CAS No.

    1633350-06-7

    SMILES

    NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)C(C5CCN(C(C=C)=O)CC5)CCN2)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.70%

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    Inquiry Information

    Product Name:
    (±)-Zanubrutinib
    Cat. No.:
    HY-101474
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