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    GNF-5
    GNF-5

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0674
    CAS #: 778277-15-9Purity ≥98%

    Description: GNF-5, a GNF-2 analog with improved pharmacokinetic properties,  is a novel, potent, selective and allosteric/non-ATP competitive Bcr-Abl inhibitor with IC50 of 220 nM for wild-type Abl. 

    References: Nature. 2010 Jan 28;463(7280):501-6; J Med Chem. 2010 Oct 14;53(19):6934-46.

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    Molecular Weight (MW)418.37
    FormulaC20H17F3N4O3
    CAS No.778277-15-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL (198.4 mM)
    Water: <1 mg/mL
    Ethanol: 20 mg/mL warmed (47.8 mM)
    Other infoChemical Name: N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
    InChi Key: IIQUYGWWHIHOCF-UHFFFAOYSA-N
    InChi Code: InChI=1S/C20H17F3N4O3/c21-20(22,23)30-16-6-4-15(5-7-16)27-18-11-17(25-12-26-18)13-2-1-3-14(10-13)19(29)24-8-9-28/h1-7,10-12,28H,8-9H2,(H,24,29)(H,25,26,27)
    SMILES Code: O=C(NCCO)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1
    SynonymsGNF 5; GNF5; GNF-5; 


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    In Vitro

    In vitro activity: GNF-5, when used in combination with imatinib or nilotinib, suppresses the emergence of resistance mutations in vitro, and displays additive inhibitory activity in biochemical and cellular assays against Bcr-Abl T315I mutant. GNF-5 shows potent antiproliferative activity with EC50 of 430 nM and 580 nM against wt-Bcr-Abl and E255K mutant Bcr-Abl transformed cells, respectively.


    Kinase Assay: The ATP/NADH-coupled assay system in a 96-well format is used to determine the initial velocity of Abl tyrosine kinase catalyzed peptide phosphorylation. The reaction mixture contained 20 mM Tris-HCl, (pH 8.0), 50 mM NaCl, 10 mM MgCl2, 2 mM PEP [2-(Phosphonooxy)- 2-propenoic acid) and 20 μg Abl peptide substrate (EAIYAAPFAKKK), fixed or varied (to determine inhibitor kinetic parameters) concentration of inhibitor applied, 1/50 of the final reaction mixture volume of PK/LDH enzyme (pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle), 160 μM NADH, 0.16 μM Abl, and ATP added last to start the reaction. Absorbance data are collected every 20s at 340 nm using a SpectraMax M5 Microplate Reader. 


    Cell Assay: Ba/F3.p210 cells are obtained by transfecting the IL-3-dependent murine hematopoietic Ba/F3 cell line with a pEYK vector containing p210BCR-ABL and Bcr-Abl mutations. All cell lines are cultured with 5% CO2 at 37 °C in RPMI 1640 with 10% fetal bovine serum (FBS) and supplemented with 1% l-glutamine. Parental Ba/F3 cells are similarly cultured with 10% WEHI-conditioned medium as a source of IL-3. Transfected cell lines are cultured in media supplemented with 25 μg/mL zeocin. The 48 h cell proliferation studies are obtained using the CellTiter-Glo assay.

    In VivoGNF-5 (100 mg/kg ) displays efficacy on wild-type and T315I Bcr-Abl dependent proliferation in xenograft and bone marrow transplantation models. Moreover, a combination of GNF-5 (75 mg/kg) with nilotinib (50 mg/kg) results in improved overall survival in a T315I Bcr-Abl BMT model. 
    Animal modelBa/F3.p210 xenograft mouse model
    Formulation & DosageDissolved in PEG400/saline (1:1); 100 mg/kg ; p.o.
    References

    Nature. 2010 Jan 28;463(7280):501-6; J Med Chem. 2010 Oct 14;53(19):6934-46.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    GNF-5

    Cellular and enzymatic inhibition of wild-type and mutants by combination treatments. Nature. 2010 Jan 28;463(7280):501-6.

    GNF-5

    In vivo efficacy studies with GNF-5 on wild-type and T315I Bcr-Abl dependent proliferation in xenograft and bone marrow transplantation models. Nature.2010 Jan 28;463(7280):501-6.

    GNF-5

    Hydrogen exchange mass spectrometry upon binding of GNF-5 to Abl. Nature. 2010 Jan 28;463(7280):501-6.


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