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...

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

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...

Description: Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively. Target: HER, EGFR. Smiles: N(C=1C2=C(C=C(OCC)C(NC(/C=C/CN(C)C)=O)=C2)N=CC1C#N)C3=CC(Cl)=C(OCC4=CC=CC=N4)C=C3. References: Canonici A, et al. Neratinib overcomes...