HKI-357
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].
Product Specifications
CAS Number
[848133-17-5]
UNSPSC
12352005
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/hki-357.html
Purity
99.24
Solubility
DMSO : 100 mg/mL (ultrasonic)
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
Molecular Formula
C31H29ClFN5O3
Molecular Weight
574.05
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
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
EGFR/ErbB1/HER1; ErbB2/HER2
Available Sizes
Curated Selection
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