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Epertinib

CAT: 0804-HY-107367Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-107367Size:1 Each
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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.
CAS Number
908305-13-5
Product Name Alternative
S-22611
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/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 Formula
C30H27ClFN5O3
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)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
EGFR/ErbB1/HER1; ErbB2/HER2; ErbB4/HER4

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MBS3840043-01Epertinib
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A13777-50Epertinib 50mg
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A13777-25Epertinib 25mg
A13777-10Epertinib 10mg
A13777-100Epertinib 100mg
A21950-100Epertinib hydrochloride 100mg
A21950-25Epertinib hydrochloride 25mg

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