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17α-[4,4-difluoro-8-(4-ethynylphenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene]-testosterone

Development stage
Preclinical
Lead developer
University of Coimbra
Modality
Small Molecules
01

Overview

17α-[4,4-difluoro-8-(4-ethynylphenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene]-testosterone is a fluorescently labeled androgen conjugate designed for theranostic applications in oncology. It consists of a testosterone scaffold linked at the 17α position to a BODIPY (4,4-difluoro-4-bora-3a,4a-diaza-s-indacene) fluorophore via an ethynylphenyl spacer. This molecular probe is utilized to visualize and study the uptake of androgens in cancer cells, specifically those expressing the androgen receptor (AR), such as LNCaP and PC-3 prostate cancer cells. The conjugate is internalized through energy-dependent endocytic pathways, including clathrin- and caveolae-mediated endocytosis. Beyond its role as an imaging agent, it exhibits potential as a photosensitizer for photodynamic therapy (PDT), where visible light irradiation triggers cytotoxic effects in targeted cancer cells.

Other names
testosterone-BODIPY conjugate17α-ethynylphenyl-BODIPY-testosterone
02

Targets

AR (Adrenergic receptors)

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