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Epertinib Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5753103

Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48nM, 7.15nM, and 2.49nM). It displays a strong antitumor activity. More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Epertinib, Inhibitor
Full Product Name
Epertinib
Product Synonym Names
S-22611
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
560.02
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
Formula
C30H27ClFN5O3
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
CAS Number
908305-13-5
Target & IC50
EGFR: ic50 1.48nM
HER2: ic50 2.49nM
HER4: ic50 7.15nM
In Vitro
Epertinib displays antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days (ED50:10.2mg/kg). Epertinib (50mg/kg, p.o.) is four times more potent activity than GW572016 and completely inhibits the growth of cancer cells in mice [1] and it also obviously decreases the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model [2].

Structure of Epertinib, inhibitor

Epertinib Inhibitor – Cat# MBS5753103

Product References and Citations for Epertinib, inhibitor

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.
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.
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.
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.

Other Notes

Small volumes of Epertinib, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Epertinib purchase

MBS5753103 is an inhibitor targeting Epertinib.
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