Description
Desmethyl erlotinib is a metabolite of erlotinib . Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC
50 = 2.5 μM). This inhibits tumor growth in human head and neck carcinoma HN5 tumor xenografts in mice with an ED
50 value of 9 mg/kg. Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC
50 = 4.6 μM) and JAK2 mutant JAK2
V617F positive hematopoietic progenitor cells (IC
50 = 5 μM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia. Formulations containing erlotinib have been used to treat certain forms of cancer, including non-small cell lung cancer.
Uses
OSI-420 (Desmethyl Erlotinib,CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells.
References
[1] zhang w1, siu ll, moore mj, chen ex.simultaneous determination of osi-774 and its major metabolite osi-420 in human plasma by using hplc with uv detection. j chromatogr b analyt technol biomed life sci. 2005 jan 5;814(1):143-7.
[2] bonomi p. erlotinib: a new therapeutic approach for non-small cell lung cancer.expert opin investig drugs. 2003 aug;12(8):1395-401.
