Description: Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent, selective dual inhibitor of EGFR and HER2, with IC50 values of 13 nM and 38 nM, respectively. Target: HER, EGFR. Smiles: OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)\C=C\[C@H]1CCCN1C. References: Li X,...

An EGFR and HER2 inhibitor (IC50s = 13 and 38 nM, respectively), selectively inhibits the proliferation of HER2+ BT474 and SKOV3 cells (IC50s = 5.1 and 43 nM, respectively) over HER2- MDA-MB-231 cells (IC50 = 3,500 nM), decreases tumor growth without affecting body weight in BT474 and SKOV3 mouse xenograft models at...