Home Angiogenesis Bcr-Abl inhibitor GNF-5 For research use only.

GNF-5

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

GNF-5 Chemical Structure

GNF-5 Chemical Structure

CAS: 778277-15-9

Selleck's GNF-5 has been cited by 13 Publications

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Purity & Quality Control

Batch: S752601 DMSO] 83 mg/mL] false] Ethanol] 20 mg/mL] false] Water] Insoluble] false Purity: 99.46%
99.46

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Biological Activity

Description GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
Targets
Bcr-Abl [1]
220 nM
In vitro
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models Ba/F3.p210 xenograft mouse model
Dosages ~100 mg/kg bid
Administration p.o.

Chemical Information & Solubility

Molecular Weight 418.37 Formula

C20H17F3N4O3
CAS No. 778277-15-9 SDF Download GNF-5 SDF
Smiles C1=CC(=CC(=C1)C(=O)NCCO)C2=CC(=NC=N2)NC3=CC=C(C=C3)OC(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (198.38 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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