Epertinib hydrochloride (Standard)  (Synonyms: S-22611 hydrochloride (Standard))

Epertinib hydrochloride (Standard) (S-22611 hydrochloride (Standard)) is the analytical standard of Epertinib (hydrochloride) (HY-107367A). This product is intended for research and analytical applications. Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine K_inase inhibitor of EGFR, HER4 and HER2, with IC₅₀s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity^[1][2]. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50: 1.48 nM (EGFR), 7.15 nM (HER2), 2.49 nM (HER4)^[1]

596.48

C₃₀H₂₈Cl₂FN₅O₃

2071195-74-7

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.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. 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.  [Content Brief]

  [2]. 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.  [Content Brief]