Description
Pyrotinib dimaleate is a potent and selective dual inhibitor of EGFR/HER2 with IC50s of 13 and 38 nM, respectively.InformationPyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor ofEGFRandHER2with IC50 of 0.013 µM and 0.038 µM, respectively.TargetsEGFR (Cell-free assay); HER2 (Cell-free assay) 0.013 µM; 0.038 µMIn vitroPyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles.In vivoPyrotinib (SHR1258) displays robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.Cell Research(from reference)Cell lines：A431, SK-BR-3, NCI-N87 Concentrations：6-7 concentrations (not specific) Incubation Time：72 h