纯度:>98% by HPLC;NMR (Conforms)
分子式:C30H29ClN6O3
分子量:557.05
溶剂:DMSO (4 mg/ml, warm)
性状:White solid
存储:-20°C
Activity (short version):Dual EGFR and HER2 inhibitor
Function / Pharmacology:Neratinib is a potent, irreversible inhibitor of HER2/ErbB2 receptor tyrosine kinase and EGFR kinase (IC50’s= 59 nM and 92 nM, respectively). It suppresses receptor autophosphorylation and proliferation, blocks cell-cycle progression and inhibits HER2 signaling in of EGFR-dependent cancer cells and tumor xenograft models.1 Neratinib inhibits proliferation of gefitinib-resistant non-small cell lung cancer cells expressing mutant EGFR.2 Synergizes with dasatinib in HER2-positive cancer cells and xenografts.3 It’s been shown to also inhibit MST1 (IC50 = 37.7 nM).4