PSMA-IN-2, an inhibitor of PSMA with a K i value of 1.07 nM, exhibits favorable in vivo NIR imaging (λ EM = 1088 nm, λ ex = 808 nm) and is useful for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice [1].

PSMA:1.07 nM (Ki)

PSMA-IN-2 (compound 24) (0.85 mg/kg, i.v., 24 h) is confirmed by NIR-II imaging to bind specifically to PSMA in vivo [1]. In 22Rv1 xenograft models [1], following an intravenous injection at a dosage of 0.85 mg/kg, the compound was excreted from the blood pool, leading to increased signal intensity in 22Rv1 xenografts over time as the background signal weakened under 808 nm laser irradiation (1100 nm long-pass filter, 400 ms), with inhibition ranging from 38% to 52% based on semi-quantitative data DCFPyL in tumors.