Epertinib

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, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target:IC50: 1.48 nM (EGFR), 7.15 nM (HER2), 2.49 nM (HER4)^[1] In Vitro:Epertinib inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC₅₀ values of 4.5 and 1.6 nM, respectively^[2].
Epertinib shows inhibitory activity against MDA-MB-361 cell, with an IC₅₀ of 26.5 nM^[1].
Epertinib (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2^[2]. In Vivo:Epertinib (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity^[1].
Epertinib (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume^[1].
Epertinib (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner^[2].