Neratinib is a dual inhibitor of EGFR and HER2 (IC50s = 92 and 59 nM, respectively). 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...

Solubility: Soluble in DMSO at 2 mg/mL with warming, very poorly soluble in ethanol, very poorly soluble in water, maximum solubility in plain water is estimated to be about 5-20 µM, buffers, serum, or other additives may increase or decrease the aqueous solubility. Neratinib, also known as HKI-272, is considered to...

Neratinib is a cell-permable, irreversible, selective inhibitor of the HER2 kinase (IC50=59nM) and EGFR (IC50=92nM) by preventing phosphorylation of these proteins by their respective kinases. It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other...

It is an orally active, irreversible tyrosine kinase inhibitor of the HER-2 and EGFR.