HKI 357
Names
[ CAS No. ]:
848133-17-5
[ Name ]:
HKI 357
[Synonym ]:
HKI 357
L-733,060 hydrochloride
UNII-39R3638KZ6
Biological Activity
[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].
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C31H29ClFN5O3
[ Molecular Weight ]:
574.04500
[ Exact Mass ]:
573.19400
[ PSA ]:
106.23000
[ LogP ]:
6.74798