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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Angiogenesis>Bcr-Abl inhibitors>GNF-5
GNF-5
  • GNF-5

GNF-5 NEW

Price $30 $47 $81
Package 10mg 25mg 50mg
Supply Ability: 10g
Update Time: 2026-04-22

Product Details

Product Name: GNF-5 CAS No.: 778277-15-9
Purity: 99.93% Supply Ability: 10g
Release date: 2026/04/22

Product Introduction

Bioactivity

NameGNF-5
DescriptionGNF-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.
Cell ResearchBa/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)
Kinase AssayKinetic 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 vitroConcurrent 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 vivoGNF-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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility InformationEthanol : 16 mg/mL (38.24 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.78 mM), Sonication is recommended.
DMSO : 16.67 mg/mL (39.85 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsSARS-CoV | SARSCoV | pharmacokinetic | Inhibitor | inhibit | GNF-5 | GNF5 | GNF-2 | Chronic myelogenous leukemia (CML) | cancer | Bcr-Abl | BcrAbl
Inhibitors RelatedEIDD-1931 | Remdesivir | Molnupiravir | Silymarin | Umifenovir hydrochloride | Hydroxychloroquine | Ritonavir | Chloroquine phosphate | Dasatinib | Dexamethasone acetate | α-Cyclodextrin | Dexamethasone
Related Compound LibrariesTarget-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Hematonosis Compound Library | Anti-Viral Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Anti-Infection Compound Library | Anti-Cancer Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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TargetMol Chemicals Inc.

6YR United StatesUnited States
  • Since: 2011-01-07
  • Address: 36 Washington Street, Wellesley Hill, MA
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