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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
GNF 5 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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 |
Molarity Calculator
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Product Datasheets
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
Keywords: GNF 5, supplier, GNF5, Bcr-Abl, kinase, allosteric, inhbitors, inhibits, selective, bcrabl, bcr, abl, fusion, philadelphia, chromosome, chronic, myeloid, leukemia, leukaemia, CML, allosteric, Abl, Kinase, Abl, Kinase, Tocris Bioscience
