Neratinib
Dual EGFR and HER2 inhibitor / 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
Biochemicals & reagents
698387-09-6
HKI-272
1 Rabindran et al. (2004), Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase; Cancer Res. 64 3958 2 Kwak et al. (2005), Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib; Proc. Natl. Acad. Sci. USA 102 7665 3 Conlon et al. (2024), Neratinib plus Dasatinib is highly synergistic in HER2-positive breast cancer in vitro and in vivo; Trans. Oncol. 49 102073 4 Yun et al. (2008), The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP; Proc. Natl. Acad. Sci. USA 105 20770
-20°C
TARGET: Kinase -- PATHWAY: EGF; Proliferation -- DISEASE AREA: Cancer