|
Biological Activity:
An irreversible tyrosine kinase inhibitor with activity against HER2 and EGFR kinases; a therapeutic agent under investigation for the treatment breast cancer and other solid tumours.
References: online 12
SK Rabindran et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004, 64(11), 3958–65. [online]
Y Minami et al. The major lung cancer-derived mutants of ERBB2 are oncogenic and are associated with sensitivity to the irreversible EGFR/ERBB2 inhibitor HKI-272. Oncogene 2007, 26(34), 5023–7. [online]
A Ocaña and E Amir. Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions. Cancer Treat Rev. 2009, 5(8), 685-691. [online]
Chemical Name: (2E)-N-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
|