1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl

GZD824 

Cat. No.: HY-15666 Purity: 98.73%
Handling Instructions

GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

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

GZD824 Chemical Structure

GZD824 Chemical Structure

CAS No. : 1257628-77-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 141 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

    GZD824 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2018 May 25;1865(9):1173-1186.

    Cell lysates are prepared from HCT-116 cells transfected with Flag-Vector or Flag-YY1. Twenty-four hours following transfection cells are treated with GZD824 with the indicated concentration for 4 h prior to 200 μM Pervanadate treatment for 30 min. Lysates are subjected to immunoprecipitation using α-Flag M2 resin followed by Western blotting.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. IC50 Value: 0.34/0.68 nM(Bce-Abl wt/T315I) [1] Target: Bcr-Abl in vitro: GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. It also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy. in vivo: GZD824 induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I) [1]. Clinical trial: GZD824 is on the way of unknown clinical status.

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.8777 mL 9.3886 mL 18.7772 mL
    5 mM 0.3755 mL 1.8777 mL 3.7554 mL
    10 mM 0.1878 mL 0.9389 mL 1.8777 mL
    Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    532.56

    Formula

    C₂₉H₂₇F₃N₆O

    CAS No.

    1257628-77-5

    SMILES

    O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN=C(NN=C5)C5=C4)=C3

    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

    10 mM in DMSO

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

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    Product Name:
    GZD824
    Cat. No.:
    HY-15666
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