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

(±)-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
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 140 In-stock
Estimated Time of Arrival: December 31
10 mg USD 220 In-stock
Estimated Time of Arrival: December 31
50 mg USD 880 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of (±)-Zanubrutinib:

Top Publications Citing Use of Products

Publications Citing Use of MCE (±)-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

    • Purity & Documentation

    • References

    • Customer Review

    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].
    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
    Shipping

    Room temperature in continental US; may vary elsewhere
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (63.62 mM)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.70%

    COA (135 KB) HNMR (351 KB) LCMS (358 KB)

    Handling Instructions (2659 KB)
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