1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl
  3. GZD824

GZD824 (Synonyms: HQP1351)

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

GZD824 (HQP1351) is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl (WT) and Bcr-Abl (T315I) with IC50s 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
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE GZD824

    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.
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    Description

    GZD824 (HQP1351) is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl (WT) and Bcr-Abl (T315I) with IC50s of 0.34 nM and 0.68 nM, respectively[1].

    IC50 & Target

    IC50: 0.34/0.68 nM (Bce-Abl wt/T315I)[1]

    In Vitro

    GZD824 (HQP1351) potently suppresses proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC50 values of 0.2 and 0.13 nM, respectively[1].

    In Vivo

    GZD824 induces tumor regression in mouse xenograft tumor models driven by Bcr-Abl (WT) or the mutants and significantly improves the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I)[1].

    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

    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 : ≥ 100 mg/mL (187.77 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.75 mg/mL (5.16 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.75 mg/mL (5.16 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.75 mg/mL (5.16 mM); Clear solution

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

    GZD824 | HQP1351 | GZD 824 | GZD-824 | HQP 1351 | HQP-1351 | Bcr-Abl | Inhibitor | inhibitor | inhibit

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