GNF 5

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Description: Selective allosteric inhibitor of Bcr-Abl; analog of GNF 2 (Cat. No. 4399)
Chemical Name: N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for GNF 5

GNF 5 is a selective, non-ATP competitive allosteric inhibitor of Bcr-Abl (IC50 = 220 nM for wild-type Abl). Binds the myristate-binding site of Abl. Acts in combination with nilotinib to inhibit T315I Bcr-Abl in vitro and in vivo. Analog of GNF 2 (Cat. No. 4399). GNF 5 decreases mitochondrial function in lung cancer cells.

External Portal Information for GNF 5

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GNF 5 is reviewed on the chemical probes website.

Compound Libraries for GNF 5

GNF 5 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for GNF 5

M. Wt 418.37
Formula C20H17F3N4O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 778277-15-9
PubChem ID 44129660
InChI Key IIQUYGWWHIHOCF-UHFFFAOYSA-N
Smiles O=C(NCCO)C1=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GNF 5

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.84 100

Preparing Stock Solutions for GNF 5

The following data is based on the product molecular weight 418.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.39 mL 11.95 mL 23.9 mL
5 mM 0.48 mL 2.39 mL 4.78 mL
10 mM 0.24 mL 1.2 mL 2.39 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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References for GNF 5

References are publications that support the biological activity of the product.

Zhang et al (2010) Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 463 501 PMID: 20072125

Iacob et al (2011) Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One 6 e15929 PMID: 21264348

Deng et al (2010) Expanding the diversity of allosteric Bcr-Abl inhibitors. J.Med.Chem. 53 6934 PMID: 20828158

Luttman et al (2021) ABL allosteric inhibitors synergize with statins to enhance apoptosis of metastatic lung cancer cells. Cell Rep. 37 109880 PMID: 34706244


If you know of a relevant reference for GNF 5, please let us know.

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Citations for GNF 5

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Literature in this Area

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