The first Pt(II) tetrazine complex, trans-[PtCl₂(dmso)(CH₃-Tz-Bz-NH₂)] (1), is reported, showing good cytotoxicity against MDA-MB-231 cells and undergoing IEDDA reactions with TCO and BCN derivatives. A live-cell IEDDA reaction in MDA-MB-231 cells with a BCN-bearing BF₂-azadipyrromethene fluorophore is tracked via FLIM, owing to a 0.3 ns lifetime shift.

The development of the first Pt(II) tetrazine complex, trans-[Pt(II)Cl₂(dmso)(CH₃-Tz-Bz-NH₂)] (1), is reported, which exhibits good in vitro cytotoxicity against MDA-MB-231 cells and succesfully undergoes inverse electron demand Diels–Alder (IEDDA) reactions with trans-cyclooctene (TCO) and bicyclononyne (BCN) derivates in solution. We demonstrate a live-cell IEDDA reaction of 1 with a BF₂-azadipyrromethene fluorophore (NIR-AZA) posessing a BCN handle. A live-cell bioorthogonal reaction is established using fluorescence lifetime imaging microscopy (FLIM), through a fluorescence lifetime change of 0.3 ns from BF₂-azadipyrromethene fluorophore starting material to IEDDA Pt fluorophore reaction product. As there is a distinct difference in fluorescence lifetimes between starting material and product, this approach removes the necessity for designing challenging off to on fluorogenic Pt probes and washing steps when developing bioorthogonal cell-imaging strategies for Pt complexes.