For research use only. Not for therapeutic Use.
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer[1][2].
GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 µM but no inhibition for myristate site mutant E505K (IC50 ＞10 µM)[1].
GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters[1].
GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses[1].
GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo[1].
| Catalog Number | I004865 |
| CAS Number | 778277-15-9 |
| Synonyms | N-(2-hydroxyethyl)-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide |
| Molecular Formula | C20H17F3N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H17F3N4O3/c21-20(22,23)30-16-6-4-15(5-7-16)27-18-11-17(25-12-26-18)13-2-1-3-14(10-13)19(29)24-8-9-28/h1-7,10-12,28H,8-9H2,(H,24,29)(H,25,26,27) |
| InChIKey | IIQUYGWWHIHOCF-UHFFFAOYSA-N |
| SMILES | C1=CC(=CC(=C1)C(=O)NCCO)C2=CC(=NC=N2)NC3=CC=C(C=C3)OC(F)(F)F |
| Reference | [1]. Zhang J, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6. [2]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. |
