Source:http://linkedlifedata.com/resource/umls/id/C1454298
PDQ: An orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile, irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. HKI-272 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. HKI-272 also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=453548&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=453548&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBr