HKI 357

CAS NO.：848133-17-5
Empirical Formula: C31H29ClFN5O3
Molecular Weight: 574.05
MDL number: MFCD26792555
SAFETY DATA SHEET (SDS)
Update Date: 2026-04-21 10:31:43

What is HKI 357?

Biological Activity

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50 of 34 nM and 33 nM, respectively. It can inhibit EGFR autophosphorylation (detected at Y1068), and AKT and MAPK phosphorylation.

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. HKI-357 is also 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.

Western Blot Analysis

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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.

Properties of HKI 357

Boiling point:	747.6±60.0 °C(Predicted)
Density	1.34±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble to 100 mM in DMSO and to 25 mM in ethanol
form	Powder
pka	12.37±0.43(Predicted)
color	Off-white to yellow

Safety information for HKI 357

Computed Descriptors for HKI 357

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