Molecular Weight(MW): 418.37
GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
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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.
Purity & Quality Control
Choose Selective Bcr-Abl Inhibitors
|Description||GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.|
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. 
|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. |
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.
|In vitro||DMSO||83 mg/mL (198.38 mM)|
|Ethanol||20 mg/mL warmed (47.8 mM)|
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