New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone–cycloalkyne click reaction†
Mylène
Richard, 
a
Vu Long
Tran,
a
Davide
Audisio,
b
Bertrand
Kuhnast,
a
Frédéric
Taran
*b
and
Simon
Specklin
*a
a
Vu Long
Tran,
a
Davide
Audisio,
b
Bertrand
Kuhnast,
a
Frédéric
Taran
*b
and
Simon
Specklin
*a
Abstract
We report the first pretargeting in vivo study using the Strain-Promoted Sydnone–Alkyne Cycloaadition (SPSAC) reaction. The injection of a fluorine-18 labeled cyclooctyne three days after cetuximab bearing chlorosydnone moieties allowed a significant detection of the tumor by PET imaging suggesting an efficient click reaction inside the tumoral site. With a kinetic constant superior to 300 M−1 s−1, the SPSAC reaction might be an interesting tool, in addition to tetrazine-cyclooctene ligation, for in vivo chemistry.
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