HKI-357 (dimaleate)
HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation[1].
Product Specifications
CAS Number
915942-25-5
UNSPSC
12352005
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/hki-357-dimaleate.html
Smiles
OC(/C=C\C(O)=O)=O.CCOC(C(NC(/C=C/CN(C)C)=O)=C1)=CC2=C1C(NC3=CC(Cl)=C(C=C3)OCC4=CC(F)=CC=C4)=C(C#N)C=N2.OC(/C=C\C(O)=O)=O
Molecular Formula
C39H37ClFN5O11
Molecular Weight
806.19
References & Citations
[1]Kwak EL, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A. 2005 May 24;102 (21) :7665-70.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 1
Frequently Asked Questions
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