HKI-357

SKU: orb1309572

Description

HKI-357 is an irreversible dual inhibitor targeting EGFR and ERBB2 with IC50 values of 34 nM and 33 nM, respectively. It effectively blocks EGFR autophosphorylation at Y1068 and downstream AKT and MAPK signaling. This compound is a valuable research tool for investigating oncogenic receptor tyrosine kinase pathways in both in vitro and in vivo cancer models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 848133-17-5
• MW: 574.05
• Purity: 95.11%
• Formula: C₃₁H₂₉ClFN₅O₃
• SMILES: CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4cccc(F)c4)c(Cl)c3)c2cc1NC(=O)\C=C\CN(C)C
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.48 mM);DMSO:30 mg/mL (52.26 mM)

Bioactivity

• Target IC50:
  ErbB2:33 nM|EGFR:34 nM
• In Vitro:
  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.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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ErbB-1, ERBB2, ErbB2, Epidermal growth factor receptor, EGFR, HER1, HKI 357, HKI357, HKI-357, inhibit, Inhibitor, NSCLCs

Compound Identifiers

PubChem CID

11238512