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Considering the well\u2010known implications of protein kinases in cancer and the therapeutic issues associated with protein kinase inhibitors, the photopharmacology is seen as an innovative and alternative solution with great potential in oncology. In this context, we developed the first photocaged TAM kinase inhibitors based on <jats:bold>UNC2025<\/jats:bold>, a first\u2010in\u2010class small molecule kinase inhibitor. These prodrugs showed good stability in biologically relevant buffer and rapid photorelease of the photoremovable protecting group upon UV\u2010light irradiation (&lt;10\u2005min.). These light\u2010activatable prodrugs led to a 16\u2010fold decrease to a complete loss of kinase inhibition, depending on the protein and the position at which the coumarin\u2010type phototrigger was introduced. The most promising candidate was the <jats:italic>N,O<\/jats:italic>\u2010dicaged compound, showing the superiority of having two photolabile protecting groups on <jats:bold>UNC2025<\/jats:bold> for being entirely inactive on TAM kinases. Under UV\u2010light irradiation, the <jats:italic>N,O<\/jats:italic>\u2010dicaged compound recovered its inhibitory potency in enzymatic assays and displayed excellent antiproliferative activity in RT112\u2005cell lines.<\/jats:p>","DOI":"10.1002\/cbic.202300855","type":"journal-article","created":{"date-parts":[[2024,2,16]],"date-time":"2024-02-16T09:09:12Z","timestamp":1708074552000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Light\u2010Activatable Photocaged UNC2025 for Triggering TAM Kinase Inhibition in Bladder Cancer"],"prefix":"10.1002","volume":"25","author":[{"given":"Chlo\u00e9","family":"Breton\u2010Patient","sequence":"first","affiliation":[{"name":"Institut Curie Universit\u00e9 PSL CNRS UMR9187, Inserm U119  91400 Orsay France"},{"name":"Universit\u00e9 Paris-Saclay CNRS UMR9187, Inserm U119  91400 Orsay 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