GNF-5

SKU: orb1307410

Description

GNF-5 is a non-ATP competitive Bcr-Abl inhibitor with an IC50 of 0.22 µM against wild-type Abl. As a pharmacokinetically improved analog of GNF-2, it is a valuable chemical probe for studying kinase-independent oncogenic signaling in chronic myeloid leukemia research, both in vitro and in vivo.

Research Area

Cardiovascular Research, Infectious Disease & Virology, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	778277-15-9
MW	418.37
Purity	99.98%
Formula	C₂₀H₁₇F₃N₄O₃
SMILES	N(C1=CC(=NC=N1)C2=CC(C(NCCO)=O)=CC=C2)C3=CC=C(OC(F)(F)F)C=C3
Target	SARS-CoV,Bcr-Abl
Solubility	Ethanol:16 mg/mL (38.24 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.78 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:16.67 mg/mL (39.85 mM)

Bioactivity

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Target IC50	BCR-ABL:0.22±0.1 μM
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. Read more...
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. Read more...
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) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Chronic myelogenous leukemia (CML), Bcr-Abl, BcrAbl, cancer, GNF5, GNF-5, GNF 5, GNF-2, Inhibitor, inhibit, pharmacokinetic, SARSCoV, SARS-CoV

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Compound Identifiers

PubChem CID

44129660 ↗

Key Properties

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No computed properties available.

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GNF-5 (orb1307410)

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Purity:	>98%(HPLC)
CAS Number:	778277-15-9
MW:	418.4
Formula:	C₂₀H₁₇F₃N₄O₃

GNF-5

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Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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