Neratinib

Overview

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.

Application

Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cardiovascular and blood system | EGFR

Product Information

• Catalog No.: B0084-347125
• CAS No.: 698387-09-6
• Molecular Formula: C30H29ClN6O3
• Molecular Weight: 557.04
• Purity: >98%
• Storage: Store at 2-8 °C
• Solubility: Soluble in Chloroform (Slightly), DMSO (Slightly, Heated, Ultrasonic), Methanol (Slightly, Heated)

Source

Original product source