1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. HKI-357

HKI-357 

Cat. No.: HY-103443
Handling Instructions

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.

For research use only. We do not sell to patients.

HKI-357 Chemical Structure

HKI-357 Chemical Structure

CAS No. : 848133-17-5

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10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1]

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.
Clinical Trial
Molecular Weight

574.05

Formula

C₃₁H₂₉ClFN₅O₃

CAS No.

848133-17-5

SMILES

O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1)/C=C/CN(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

HKI-357HKI357HKI 357EGFREpidermal growth factor receptorErbB-1HER1ERBB2NSCLCsInhibitorinhibitorinhibit

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HKI-357
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HY-103443
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