For research use only.

Catalog No.S7526

4 publications

GNF-5 Chemical Structure

Molecular Weight(MW): 418.37

GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.

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Selleck's GNF-5 has been cited by 4 publications

2 Customer Reviews

  • IC50 values for GNF-5-treated Ba/F3 cells expressing BCR-ABL1 or ABL1 1b mutants (a) described to confer ABL001 resistance in BCR-ABL1, (b) identified by mutagenesis screen. after 48 hours. Error bars represent SD of triplicates from three independent experiments. Significance levels in comparison with BCR-ABL1 are indicated (NS, not significant; *P<0.05, **P<0.01, ***P<0.001, two-tailed unpaired t-test).

    Leukemia, 2017, 31(5):1096-1107. GNF-5 purchased from Selleck.

    Cell viability of K562/IR cells and their parental cell lines after exposure to different concentrations of (I) GNF-5 for 72 h. These results are representative of 5 independent experiments. *p < 0.01 vs. untreated K562 cells as assessed with Dunnett's test.

    Oncotarget, 2017, 8(24):38717-38730. GNF-5 purchased from Selleck.

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Biological Activity

Description GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
Bcr-Abl [1]
220 nM
In vitro

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. [1] 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. [2]

In vivo GNF-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. [1]


Kinase Assay:[1]
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Kinetic characterization of Abl inhibition:

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 Research:[2]
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  • Cell lines: Ba/F3.p210 cells
  • Concentrations: ~10 μM
  • Incubation Time: 48 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Ba/F3.p210 xenograft mouse model
  • Dosages: ~100 mg/kg bid
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (198.38 mM)
Ethanol 20 mg/mL warmed (47.8 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 418.37


CAS No. 778277-15-9
Storage powder
in solvent
Synonyms N/A
Smiles OCCNC(=O)C1=CC=CC(=C1)C2=CC(=NC=N2)NC3=CC=C(OC(F)(F)F)C=C3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Bcr-Abl Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID