Neratinib, also known as HKI-272 or PB272, is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.
Properties:
Density: 1.337 g/cm3
Boiling Point: 756.97ºC at 760 mmHg
Flash Point: 411.601ºC
Related Products:
Afatinib dimaleate; Bosutinib; Bosutinib Intermediates; Bosutinib Monohydrate; Saracatinib; Dasatinib; NVP-BHG712; PP1; PP2; A-966492; G007-LK; SU6656; Tirbanibulin; TPX-0005; Afatinib