Pyrotinib maleate (SHR-1258 maleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively; displays high selectivity in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and c-Met (c-Src with an IC50 of 790 nM, and others >3,000 nM); exhibits robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.
