For research use only. Not for therapeutic Use.
GNF-2（Cat No.:I004864）is a selective allosteric inhibitor of the BCR-ABL kinase, which plays a crucial role in chronic myeloid leukemia (CML) pathogenesis. Unlike ATP-competitive inhibitors, GNF-2 binds to the myristoyl pocket of the BCR-ABL protein, stabilizing its inactive conformation and reducing its oncogenic activity. This mechanism provides a novel approach for targeting imatinib-resistant forms of BCR-ABL, making GNF-2 valuable in leukemia research. Its selective inhibition of BCR-ABL without affecting other kinases highlights its potential for developing more precise cancer therapies.
| Catalog Number | I004864 |
| CAS Number | 778270-11-4 |
| Synonyms | 3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide |
| Molecular Formula | C₁₈H₁₃F₃N₄O₂ |
| Purity | ≥95% |
| Target | Bcr-Abl |
| Solubility | DMSO: ≥ 45 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 0.14 uM |
| IUPAC Name | 3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide |
| 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 |
| SMILES | C1=CC(=CC(=C1)C(=O)N)C2=CC(=NC=N2)NC3=CC=C(C=C3)OC(F)(F)F |
| Reference | </br>1:GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein. Clark MJ, Miduturu C, Schmidt AG, Zhu X, Pitts JD, Wang J, Potisopon S, Zhang J, Wojciechowski A, Hann Chu JJ, Gray NS, Yang PL.Cell Chem Biol. 2016 Apr 21;23(4):443-52. doi: 10.1016/j.chembiol.2016.03.010. PMID: 27105280 Free PMC Article</br>2:Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib. Pan X, Dong J, Shao R, Su P, Shi Y, Wang J, He L.Bioorg Med Chem Lett. 2015 Oct 1;25(19):4164-8. doi: 10.1016/j.bmcl.2015.08.013. Epub 2015 Aug 8. PMID: 26298495 </br>3:The tyrosine kinase inhibitor GNF-2 suppresses osteoclast formation and activity. Kim HJ, Yoon HJ, Choi JY, Lee IK, Kim SY.J Leukoc Biol. 2014 Feb;95(2):337-45. doi: 10.1189/jlb.0713356. Epub 2013 Oct 15. PMID: 24130113 Free Article</br>4:Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism. Khateb M, Ruimi N, Khamisie H, Najajreh Y, Mian A, Metodieva A, Ruthardt M, Mahajna J.BMC Cancer. 2012 Nov 27;12:563. doi: 10.1186/1471-2407-12-563. PMID: 23186157 Free PMC Article</br>5:p185(BCR/ABL) has a lower sensitivity than p210(BCR/ABL) to the allosteric inhibitor GNF-2 in Philadelphia chromosome-positive acute lymphatic leukemia. Mian AA, Metodieva A, Najajreh Y, Ottmann OG, Mahajna J, Ruthardt M.Haematologica. 2012 Feb;97(2):251-7. doi: 10.3324/haematol.2011.047191. Epub 2011 Nov 4. PMID: 22058195 Free PMC Article |
