GNF-2

• CAT Number: I004864
• CAS Number: 778270-11-4
• Molecular Formula: C₁₈H₁₃F₃N₄O₂
• Molecular Weight: 374.32
• Purity: ≥95%
• Target: Bcr-Abl
• Solubility: DMSO: ≥ 45 mg/mL
• Storage: 3 years -20C powder
• IC50: 0.14 uM [1]
• 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

GNF-2 (CAT: I004864) is a selective, non-ATP competitive inhibitor of Bcr-Abl kinase, which is a fusion protein associated with chronic myeloid leukemia (CML). It binds to the myristoyl pocket of Bcr-Abl and disrupts the interaction between Bcr-Abl and its downstream signaling proteins, inhibiting the proliferation and survival of CML cells. GNF-2 has shown promising results in preclinical studies, demonstrating potent antitumor activity against Bcr-Abl-positive cells. It has the potential to be developed as a targeted therapy for CML and other Bcr-Abl-driven malignancies.

Reference

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 Article2: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 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 Article4: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 Article5: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