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

GNF-5 

Cat. No.: HY-15738 Purity: >98.0%
Handling Instructions

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).

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

GNF-5 Chemical Structure

GNF-5 Chemical Structure

CAS No. : 778277-15-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 288 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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

    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

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl). IC50 Value: 0.22±0.1 uM (Wild type Abl) [1] Target: Abl GNF-5 is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 M against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site 'gatekeeper' mutant T315I.

    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.

      GNF-5 is prepared in vehicle (5% DMSO, 2% hydroxypropyl methylcellulose, 0.5% Tween-80)[2].

    References
    Molecular Weight

    418.37

    Formula

    C₂₀H₁₇F₃N₄O₃

    CAS No.

    778277-15-9

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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

    Cat. No.: HY-15738