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

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.

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GNF-5 Chemical Structure

GNF-5 Chemical Structure

CAS No. : 778277-15-9

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10 mM * 1 mL in DMSO
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Based on 4 publication(s) in Google Scholar

GNF-5 Related Antibodies

Top Publications Citing Use of Products

    GNF-5 purchased from MedChemExpress. 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].

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

    GNF-5 Related Antibodies

    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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    White to off-white

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 49 mg/mL (117.12 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3902 mL 11.9511 mL 23.9023 mL 59.7557 mL
    5 mM 0.4780 mL 2.3902 mL 4.7805 mL 11.9511 mL
    10 mM 0.2390 mL 1.1951 mL 2.3902 mL 5.9756 mL
    15 mM 0.1593 mL 0.7967 mL 1.5935 mL 3.9837 mL
    20 mM 0.1195 mL 0.5976 mL 1.1951 mL 2.9878 mL
    25 mM 0.0956 mL 0.4780 mL 0.9561 mL 2.3902 mL
    30 mM 0.0797 mL 0.3984 mL 0.7967 mL 1.9919 mL
    40 mM 0.0598 mL 0.2988 mL 0.5976 mL 1.4939 mL
    50 mM 0.0478 mL 0.2390 mL 0.4780 mL 1.1951 mL
    60 mM 0.0398 mL 0.1992 mL 0.3984 mL 0.9959 mL
    80 mM 0.0299 mL 0.1494 mL 0.2988 mL 0.7469 mL
    100 mM 0.0239 mL 0.1195 mL 0.2390 mL 0.5976 mL
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    GNF-5 Related Classifications

    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.

    Keywords:

    GNF-5778277-15-9GNF5GNF 5Bcr-AblGNF-2pharmacokineticChronic myelogenous leukemia (CML)cancerInhibitorinhibitorinhibit

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