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

Olverembatinib (Synonyms: GZD824; HQP1351)

Cat. No.: HY-15666 Purity: 99.88%
Handling Instructions

Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity.

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

Olverembatinib Chemical Structure

Olverembatinib Chemical Structure

CAS No. : 1257628-77-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 141 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 141 In-stock
Estimated Time of Arrival: December 31
Solid
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 3 publication(s) in Google Scholar

Other Forms of Olverembatinib:

Top Publications Citing Use of Products

    Olverembatinib 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

    Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib 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

    Olverembatinib shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].
    Olverembatinib selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].
    Olverembatinib 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

    Olverembatinib suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT[1].
    Olverembatinib (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].
    Olverembatinib exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].
    Olverembatinib 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

    532.56

    Formula

    C₂₉H₂₇F₃N₆O

    CAS No.
    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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    Product Name:
    Olverembatinib
    Cat. No.:
    HY-15666
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