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

GZD824 dimesylate (Synonyms: HQP1351 dimesylate)

Cat. No.: HY-15666A Purity: 99.20%
Handling Instructions

GZD824 dimesylate (HQP1351 dimesylate) is an orally bioavailable pan-Bcr-Abl inhibitor with potency against a wide range of Bcr-Abl mutants and the native enzyme (IC50=0.34 nM). GZD824 dimesylate has antitumor activity.

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

GZD824 dimesylate Chemical Structure

GZD824 dimesylate Chemical Structure

CAS No. : 1421783-64-3

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 191 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  
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of GZD824 dimesylate:

Top Publications Citing Use of Products

Publications Citing Use of MCE GZD824 dimesylate

    GZD824 dimesylate 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 dimesylate (HQP1351 dimesylate) is an orally bioavailable pan-Bcr-Abl inhibitor with potency against a wide range of Bcr-Abl mutants and the native enzyme (IC50=0.34 nM). GZD824 dimesylate has antitumor activity[1].

    IC50 & Target

    IC50: 0.68 nM (Bcr-AblT315I), 0.27 nM (Bcr-AblE255K) , 0.71 nM (Bcr-AblG250E) , 0.15 nM (Bcr-AblQ252H), 0.35 nM (Bcr-Abl H396P), 0.29 nM (Bcr-Abl M351T), 0.35 nM (Bcr-AblY253F), Bcr-AblF317L[1]

    In Vitro

    GZD824 dimesylate shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].
    GZD824 dimesylate selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].
    GZD824 dimesylate inhibits Bcr-Abl signaling in K562 (1-20 nM; 4.0 hours) and Ba/F3 stable cell lines expressing native Bcr-Abl (0.1-100 nM; 4.0 hours) or Bcr-AblT315I(0.1-100 nM; 4.0 hours)[1].

    Western Blot Analysis[1]

    Cell Line: K562 cells
    Concentration: 1 nM, 2 nM, 5 nM, 10 nM, 20nM
    Incubation Time: 4.0 hours
    Result: Inhibited Bcr-Abl signaling in K562 cell lines.
    In Vivo

    GZD824 dimesylate suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT[1].
    GZD824 dimesylate (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-AblT315I[1].
    GZD824 dimesylate exhibits a good oral bioavailability (rat 48.7%) and Cmax (i.v. 1375.6 μg/L; oral 390.5 μg/L) following administration (5 mg/kg for i.v.; 25 mg/kg for oral) in rat[1].

    Animal Model: SCID nude mice, bearing allografted Ba/F3 cells expressing Bcr-AblT315I[1]
    Dosage: 1 mg/kg, 2 mg/kg, 5.0 mg/kg, 10 mg/kg, 20 mg/kg
    Administration: Oral gavage, daily, for 10 days
    Result: Efficiently prolongs animal survival in an allograft leukemia tumor model.
    Animal Model: Rats[1]
    Dosage: 5 mg/kg for i.v.; 25 mg/kg for oral (Pharmacokinetic Analysis)
    Administration: Intravenous injection and oral administration
    Result: Oral bioavailability (48.7%), Cmax(1375.6 μg/L for i.v.; 390.5μg/L for oral), T1/2 (5.6 hour for i.v.; 10.6 hours for oral).
    Molecular Weight

    724.77

    Formula

    C₃₁H₃₅F₃N₆O₇S₂

    CAS No.

    1421783-64-3

    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.CS(=O)(O)=O.CS(=O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (172.47 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3797 mL 6.8987 mL 13.7975 mL
    5 mM 0.2759 mL 1.3797 mL 2.7595 mL
    10 mM 0.1380 mL 0.6899 mL 1.3797 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: ≥ 2.08 mg/mL (2.87 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (2.87 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (2.87 mM); Clear solution

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

    GZD824 dimesylateHQP1351 dimesylateBcr-Ablphosphorylatednonphosphorylatedbreakpointclusterregion-AbelsonlinaseimatinibresistanceBcr-Abl(T315I)Inhibitorinhibitorinhibit

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    Product Name:
    GZD824 dimesylate
    Cat. No.:
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