Epertinib
Product Specifications
UNSPSC Description
Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib shows potent antitumor activity[1][2]. Epertinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Target Antigen
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/Epertinib.html
Purity
98.0
Solubility
10 mM in DMSO
Smiles
CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[C@@H]5NCCOC5
Molecular Weight
560.02
References & Citations
[1]Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105(8):1040-8.|[2]Tanaka Y, et al. Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity. Sci Rep. 2018 Jan 10;8(1):343.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-107367/Epertinib-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-107367/Epertinib-SDS-MedChemExpress.pdf
Clinical Information
Phase 2
CAS Number
908305-13-5
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