1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl
  3. GNF-5

GNF-5 

Cat. No.: HY-15738 Purity: 99.42%
COA Handling Instructions

GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer.

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

GNF-5 Chemical Structure

GNF-5 Chemical Structure

CAS No. : 778277-15-9

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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
10 mg USD 66 In-stock
Estimated Time of Arrival: December 31
50 mg USD 198 In-stock
Estimated Time of Arrival: December 31
100 mg USD 317 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GNF-5 purchased from MCE. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183.  [Abstract]

    Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer[1][2].

    IC50 & Target

    IC50: 0.22 µM (Abl)[1]

    In Vitro

    GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 µM but no inhibition for myristate site mutant E505K (IC50 >10 µM)[1].

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

    Cell Viability Assay[1]

    Cell Line: wild type and mutant Bcr-Abl expressing Ba/F3 cells
    Concentration: 0.2, 0.8 and 1.6 μM
    Incubation Time: 48 h
    Result: Inhibited wild-type Abl in a non-ATP competitive fashion.
    In Vivo

    GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters[1].
    GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses[1].
    GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo[1].

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

    Animal Model: Male Balb/c mice[1]
    Dosage: 5 mg/kg, 20 mg/kg
    Administration: 5 mg/kg intravenously or 20 mg/kg orally
    Result:
    AUC_inf (min*ug/mL) 292.37
    AUC_inf (hrs*nM 11647
    Cmax(nM) 4386.08
    Tmax(hrs) 0.50
    Clast (nM) 636.16
    T1/2(hrs) 2.30
    Vss(L/kg) 9.18
    F (%) 44.82
    Animal Model: p210 xenograft model[1]
    Dosage: 50 or 100 mg/kg
    Administration: oral, twice daily, for 7 days
    Result: Could normalize blood counts and spleen size.
    Animal Model: Bone marrow transduction/transplantation model[1]
    Dosage: 75 mg/kg
    Administration: twice daily
    Result: Showed no significant response (alone).
    Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.
    Molecular Weight

    418.37

    Formula

    C20H17F3N4O3

    CAS No.
    SMILES

    FC(F)(F)OC(C=C1)=CC=C1NC2=NC=NC(C3=CC=CC(C(NCCO)=O)=C3)=C2

    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 : ≥ 49 mg/mL (117.12 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3902 mL 11.9511 mL 23.9023 mL
    5 mM 0.4780 mL 2.3902 mL 4.7805 mL
    10 mM 0.2390 mL 1.1951 mL 2.3902 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: ≥ 2.5 mg/mL (5.98 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    GNF-5
    Cat. No.:
    HY-15738
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