Name | (E)-N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
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Synonyms |
HKI 357
L-733,060 hydrochloride UNII-39R3638KZ6 |
Description | HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation[1]. |
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Related Catalog | |
Target |
EGFR:34 nM (IC50) ErbB2:33 nM (IC50) |
In Vitro | HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells[1]. HKI-357 also is effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation[1]. Western Blot Analysis[1] Cell Line: NCI-H1975 bronchoalveolar cell line Concentration: 0.01, 0.01, 0.1, 1 and 10 μM Incubation Time: Result: Suppressed ligand-induced EGFR autophosphorylation and its downstream signaling AKT and MAPK phosphorylation. |
References |
Molecular Formula | C31H29ClFN5O3 |
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Molecular Weight | 574.04500 |
Exact Mass | 573.19400 |
PSA | 106.23000 |
LogP | 6.74798 |