GNF 5

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Cat.No. 4908 - GNF 5 | C20H17F3N4O3 | CAS No. 778277-15-9
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

Biological Activity

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).

External Portal Information

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

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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