Authors: Flaviu Bulat1, 2, 3, Friederike Hesse1, Susana Ros1, Bala Atilli1, De-en Hu1, Connor J. Willmington-Holmes2, Dmitry Soloviev1, Franklin I. Aigbirhio3, Finian J. Leeper2, Kevin M. Brindle1, André A. Neves1
1 University of Cambridge, Cancer Research UK Cambridge Institute, Cambridge, United Kingdom
2 University of Cambridge, Department of Chemistry, Cambridge, United Kingdom
3 University of Cambridge, Wolfson Brain Imaging Centre, Cambridge, United Kingdom
Background
Cell death is an important target for imaging the early response of tumours to treatment. We have described recently 99mTc- and 111In-labelled derivatives of a phosphatidylserine-binding protein (C2Am) for imaging tumour cell death in vivo using SPECT [1].
Aims
We describe here the development and in vivo testing of a 18F-labelled derivative of C2Am for PET imaging of tumour cell death following therapy.
Methods
A one-pot, two-step automated synthesis of N-(5-[18F]fluoropentyl)maleimide (60 min, 12% RCY) has been developed. This was used to label the single cysteine present in C2Am within 30 min (Am=212±30 GBq/µmol (n=3)). Binding of [18F]FPenM-C2Am was assessed pre- and post-treatment in vivo by dynamic PET imaging and biodistribution studies.