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GNF 2
- Soluble in DMSO
- MF: C18H13F3N4O2
- MW: 374.32
Description
GNF 2 is a selective allosteric Bcr-Abl tyrosine kinase inhibitor with a reported IC50 value of 267 nM.
GNF 2 binds an allosteric site distinct from the ATP pocket and provides a chemical-genetic approach to ABL conformational regulation. It is useful for studying Bcr-Abl signaling, kinase allostery and combination strategies with ATP-competitive inhibitors.
Key Features
- Allosteric Bcr-Abl inhibitor
- Reported IC50: 267 nM
- Inactive against a broad panel of unrelated kinases in reported profiling
- Useful for studying ABL conformational regulation
Applications
- Bcr-Abl signaling and CML model research
- Allosteric kinase inhibition studies
- Combination profiling with ATP-site ABL inhibitors
- Kinase selectivity and resistance mechanism assays
More Information
| Parent CAS No. | 778270-11-4 |
|---|---|
| Chemical Name | 3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide |
| SMILES | C1C=C(C(N)=O)C=C(C2C=C(NC3C=CC(OC(F)(F)F)=CC=3)N=CN=2)C=1 |
| MFCD | MFCD09265253 |
| InChi | InChI=1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25) |
| InChiKey | WEVYNIUIFUYDGI-UHFFFAOYSA-N |
| CID | 5311510 |
| Short Description | Bcr-Abl inhibitor |
References
- FJ Adrián et al. Allosteric inhibitors of Bcr-abl–dependent cell proliferation. Nature Chem. Biol. 2006, 2, 95-102.
- J Zhang, FJ Adrián et al. Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors. Nature 2010, 463, 501-506.
- O Hantschel. Allosteric BCR-ABL inhibitors in Philadelphia chromosome-positive acute lymphoblastic leukemia: novel opportunities for drug combinations to overcome resistance. Haematol. 2012, 97(2), 157-159.
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