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

GZD824 dimesylate (Synonyms: HQP1351 dimesylate)

Cat. No.: HY-15666A Purity: 99.20%
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GZD824 dimesylate (HQP1351 dimesylate) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 dimesylate strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. 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
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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 a potent and orally active pan-Bcr-Abl inhibitor. GZD824 dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 dimesylate strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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 (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].
    GZD824 dimesylate exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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 prolonged 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 (390.5 μg/L), T1/2 (5.6 h).
    Clinical Trial
    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.:
    HY-15666A
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