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GNF-5

Catalog No. T1803 CAS 778277-15-9

Synonyms: GNF 5

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

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GNF-5, CAS 778277-15-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 32.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 78.00
50 mg	In stock	$ 135.00
100 mg	In stock	$ 198.00
200 mg	In stock	$ 359.00
500 mg	In stock	$ 593.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.98%

Purity: 99.78%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties.
Targets&IC50	BCR-ABL:0.22±0.1 μM
In vitro	Concurrent administration of GNF-5 (75 mg/kg) with nilotinib (50 mg/kg) has been shown to increase the overall survival rate in a T315I Bcr-Abl BMT model. Additionally, GNF-5 (100 mg/kg) demonstrated therapeutic efficacy against both wild-type and T315I Bcr-Abl-dependent proliferation in xenograft and bone marrow transplantation models.
In vivo	GNF-5 exhibits strong antiproliferative activities, inhibiting the proliferation of cells expressing wild-type Bcr-Abl (EC50: 430 nM) and its E255K mutant variant (EC50: 580 nM). When used in combination with nilotinib or imatinib, GNF-5 suppresses the emergence of resistant mutations in vitro and demonstrates enhanced inhibitory effects against the Bcr-Abl T315I mutant in both cell-based and biochemical assays.
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	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)

Synonyms	GNF 5
Molecular Weight	418.37
Formula	C20H17F3N4O3
CAS No.	778277-15-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 16 mg/mL (38.2 mM)

DMSO: 77 mg/mL (184 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Zhang J, et al. Nature. 2010, 463(7280), 501-506. 2. Deng X, et al. J Med Chem. 2010, 53(19), 6934-6946.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Inhibitor Library Angiogenesis related Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Metabolism Compound Library Anti-Cancer Compound Library Bioactive Compound Library Fluorochemical Library Bioactive Compounds Library Max

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Keywords

GNF-5 778277-15-9 Angiogenesis Cytoskeletal Signaling Microbiology/Virology Tyrosine Kinase/Adaptors Bcr-Abl SARS-CoV Inhibitor GNF-2 pharmacokinetic cancer GNF 5 Chronic myelogenous leukemia (CML) GNF5 inhibit inhibitor

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