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Biological Activity:
An active O-desmethyl metabolite of Erlotinib (Axon 1128), which inhibits EGFR tyrosine kinase; precursor of [11C]-labelled Erlotinib for PET study.
References:
A Broniscer et al. Plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite OSI-420. Clin. Cancer Res. 2007, 13(5), 1511-1515. [online]
Y Togashi et al. Cerebrospinal Fluid Concentration of Erlotinib and its Active Metabolite OSI-420 in Patients with Central Nervous System Metastases of Non-small Cell Lung Cancer. J. Thoracic Oncol. 2010, 5(7), 950-955. [online]
NF Smith et al. Modulation of erlotinib pharmacokinetics in mice by a novel cytochromeP450 3A4 inhibitor, BAS 100. Br. J. Cancer 2008, 98, 1630–1632. [online]
AA Memon et al. Positron Emission Tomography (PET) Imaging with [11C]-Labeled Erlotinib: A Micro-PET Study on Mice with Lung Tumor Xenografts. Cancer Res. 2009, 69(3), 873-878. [online]
Chemical Name: 2-(4-(3-ethynylphenylamino)-7-(2-methoxyethoxy)quinazolin-6-yloxy)ethanol
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