For research use only. Not for therapeutic Use.
HKI-357(CAT: I010786) is an irreversible, dual EGFR/ERBB2 (HER2) inhibitor with IC₅₀ values of 34 nM and 33 nM, respectively. It potently blocks EGFR autophosphorylation at Y1068 and downstream signaling through AKT and MAPK pathways. In NCI-H1975 cells, HKI-357 (0.01–10 μM) effectively suppresses ligand-induced EGFR activation and signaling, while also inhibiting autophosphorylation and downstream kinases in NCI-H1650 cells carrying the EGFR delE746-A750 mutation. Through its covalent binding and dual-targeted activity, HKI-357 provides a valuable pharmacological tool for studying EGFR/ERBB2 signaling, resistance mechanisms, and targeted therapeutic strategies in cancer research.
| CAS Number | 848133-17-5 |
| Synonyms | (E)-N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| Molecular Formula | C31H29ClFN5O3 |
| Purity | ≥95% |
| IUPAC Name | (E)-N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| InChI | InChI=1S/C31H29ClFN5O3/c1-4-40-29-16-26-24(15-27(29)37-30(39)9-6-12-38(2)3)31(21(17-34)18-35-26)36-23-10-11-28(25(32)14-23)41-19-20-7-5-8-22(33)13-20/h5-11,13-16,18H,4,12,19H2,1-3H3,(H,35,36)(H,37,39)/b9-6+ |
| InChIKey | NERXPXBELDBEPZ-RMKNXTFCSA-N |
| SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl)C#N)NC(=O)C=CCN(C)C |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
