产品描述:
Neratinib is a dual inhibitor of EGFR and HER2 (IC50s = 92 and 59 nM, respectively).{30796} It is selective for EGFR and HER2 over a panel of 12 kinases (IC50s = >5,000 nM) but does inhibit VEGFR2 and Src (IC50s = 800 and 1,400 nM, respectively). Neratinib inhibits the proliferation of NCI H508 colorectal cancer cells expressing wild-type or mutant forms of HER2 (IC50s = 0.2-3 nM).{30794} It reduces tumor growth in BT474 breast and SKOV3 ovarian cancer mouse xenograft models when administered at a dose of 40 mg/kg.{30796} Formulations containing neratinib have been used in the treatment of breast cancer.