Biological Activity
Allosteric inhibitor of Bcr-Abl tyrosine kinase activity (IC50 = 267 nM); inhibits proliferation and induces apoptosis in Bcr-Abl-expressing cells. Selective for Bcr-Abl over a panel of serine, threonine and tyrosine kinases. Non-ATP-competitive.
Compound Libraries
GNF 2 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 374.32 |
| Formula | C18H13F3N4O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 778270-11-4 |
| PubChem ID | 5311510 |
| InChI Key | WEVYNIUIFUYDGI-UHFFFAOYSA-N |
| Smiles | NC(C1=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=CC=C1)=O |
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 | 37.43 | 100 | |
| ethanol | 18.72 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 374.32. 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 | 2.67 mL | 13.36 mL | 26.72 mL |
| 5 mM | 0.53 mL | 2.67 mL | 5.34 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.67 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 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
Adrián et al (2006) Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat.Chem.Biol. 2 95 PMID: 16415863
Ohren & Sebolt-Leopold et al (2006) Inhibitors of Bcr-abl... breaking new ground again. Nat.Chem.Biol. 2 63 PMID: 16421581
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