Synthesis and preclinical evaluation of a selective MET kinase positron emission tomography tracer

被引：0

作者：

Lien, Vegard Torp ^{[1
,2
]}

Hauge, Emily ^{[1
,2
]}

Nuruddin, Syed ^{[2
]}

Klaveness, Jo ^{[1
]}

Olberg, Dag Erlend ^{[1
,2
]}

机构：

[1] Univ Oslo, Dept Pharm, Oslo, Norway

[2] Norwegian Med Cyclotron Ctr, Oslo, Norway

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2023年 / 66卷 / 14期

关键词：

autoradiography; fluoroethyl tosylate; in vivo evaluation; MET kinase; PET imaging; PROSTATE-CANCER; INHIBITORS;

D O I：

10.1002/jlcr.4066

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The tyrosine kinase MET (hepatocyte growth factor receptor) is activated or mutated in a wide range of cancers and is often correlated with a poor prognosis. Precision medicine with positron emission tomography (PET) can potentially aid in the assessment of tumor biochemistry and heterogeneity, which can prompt the selection of the most effective therapeutic regimes. The selective MET inhibitor PF04217903 (1) formed the basis for a bioisosteric replacement, leading to the deoxyfluorinated analog [F-18]2. [F-18]2 could be synthesized with a "hydrous fluoroethylation" protocol in 6.3 +/- 2.6% radiochemical yield and a molar activity of >50 GBq/mu mol. In vitro autoradiography indicated that [F-18]2 selectively binds to MET in PC3 tumor tissue, and in vivo biodistribution in mice showed predominantly a hepatobiliary excretion along with a low retention of radiotracer in other organs.

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收藏

页码：452 / 460

页数：9

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