Radiosynthesis of ML03, a novel positron emission tomography biomarker for targeting epidermal growth factor receptor via the labeling synthon:: [11C]acryloyl chloride

被引：39

作者：

Ben-David, I ^{[1
]}

Rozen, Y ^{[1
]}

Ortu, G ^{[1
]}

Mishani, E ^{[1
]}

机构：

[1] Hadassah Hebrew Univ Hosp, Dept Med Biophys & Nucl Med, IL-91120 Jerusalem, Israel

来源：

APPLIED RADIATION AND ISOTOPES | 2003年 / 58卷 / 02期

基金：

美国国家科学基金会;

关键词：

PET; carbon-11; acid chloride; EGFr-TK;

D O I：

10.1016/S0969-8043(02)00301-9

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

An automated procedure for the radiosynthesis of the labeling synthon [C-11]acryloyl chloride was developed and applied for labeling several N-acryl amides with carbon-11. [C-11]-6-acrylamido-4-(3,4-dichloro-6-fluoroanilino)quinazoline (ML03), a novel PET biomarker targeting the epidermal growth factor receptor tyrosine kinase (EGFr-TK) in cancer, was successfully prepared using this labeled synthon in a fully automated manner. Two other potential anticancer drugs were also labeled using the developed methodology. The potency of ML03 to inhibit autophosphorylation of EGFr-TK was evaluated by an ELISA assay indicating a low IC50 of 0.037 nM. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：209 / 217

页数：9

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