384838-84-0Relevant academic research and scientific papers
Fluorine-18 labeling of ML04 - Presently the most promising irreversible inhibitor candidate for visualization of EGFR in cancer
Dissoki, Samar,Laky, Desideriu,Mishani, Eyal
, p. 533 - 543 (2006)
Overexpression of the EGFR has been linked to cell malignancy, metastasis and poor prognosis thus making it a target for several FDA approved drugs such as Gefitinib and Erlotinib. Unfortunately, these drugs have yielded suboptimal clinical results. In order to evaluate and monitor EGFR-targeted treatment response at the molecular level, several PET biomarkers have been developed. One of the lead irreversible inhibitors (1) has been labeled with carbon-11, however the short half-life of this radioisotope limited the time window for in vivo studies. Compound 1 was successfully labeled with fluorine-18 via a multi-step radiosynthesis with 14% decay-corrected overall radiochemical yield, 98% radiochemical purity, specific activity of 1800 Ci/mmol (n = 10) at end of bombardment, and a total radiosynthesis time of 4h including purification and formulation. [18F]-1 will allow for prolonged in vivo studies including Micro-PET analysis of EGFR tumor-bearing animal models. Copyright
