Piflufolastat CAS# 1423758-00-2 N-(1S)-1-羧基-5-(6-氟-3-吡啶基)羰基胺新戊基氨基酰-L-谷氨酸

Piflufolastat F19 (DCFPyL, non-radioactive analog of ^18F-DCFPyL) is a high-affinity ligand for prostate-specific membrane antigen (PSMA) used to characterize binding and pharmacologic properties independent of radiolabeling. In preclinical binding assays, piflufolastat F19 demonstrated nanomolar affinity for PSMA (Ki ~1–2 nM) and effectively inhibited PSMA enzymatic activity in LNCaP cell lysates. It showed high selectivity versus other glutamate carboxypeptidases and displayed strong PSMA-mediated uptake in prostate cancer cells. In mouse models, piflufolastat F19 accumulated selectively in PSMA-positive xenografts with rapid clearance from non-target tissues. These results confirmed its suitability as a stable, high-affinity PSMA-targeting scaffold for imaging agent development.