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Epertinib

$220

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Products Details

Product 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.

Web ID

– HY-107367

Storage Temperature

– 4°C (Powder, protect from light)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C30H27ClFN5O3

References

– [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.

CAS Number

– 908305-13-5

Molecular Weight

– 560.02

Compound Purity

– 98.0

SMILES

– CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=NOC[C@@H]5NCCOC5

Clinical Information

– Phase 2

Research Area

– Cancer

Solubility

– 10 mM in DMSO

Target

– EGFR

Isoform

– EGFR/ErbB1/HER1;ErbB2/HER2;ErbB4/HER4

Pathway

– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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