Evaluation of the biodistribution of DUPA conjugates in vivo
(A) Whole animal imaging of animals with LNCaP (PSMA+) xenografts following systemic injection of 10 nmol DUPA-NIR at the indicated time points (n = 3, one representative mouse from each treatment shown). Pretreatment with the PSMA inhibitor, PMPA, reduced accumulation of NIR signal in LNCaP tumors. (B) Gross images of excised LNCaP tumors and whole organs visualized for NIR signal. Data are graphically represented from all animals included in the study (n = 3). ∗p < 0.05, two-tailed unpaired t test. Error bars are mean ± SD. (C) Representative whole animal imaging of mice implanted with 22Rv1 (PSMA+) or A549 (PSMA−) cells following systemic injection of DUPA-NIR. Images were acquired 1, 24, and 48 h after delivery. Red boxes represent the tumors (n = 3, one representative mouse from each treatment shown). (D) Gross images of representative excised 22Rv1 and A549 tumors and organs visualized for NIR signal. NIR signal from tumors/organs is represented graphically from all animals included in the study, (n = 3). Error bars are mean ± SD. (E) Quantification of NIR signal in LNCaP, 22Rv1, or A549 tumors normalized to NIR signal from kidneys from experiments in (B) and (D) (n = 3). ∗∗p < 0.01, one-way ANOVA. Error bars are mean ± SD. (F) Representative whole animal imaging of mice implanted with LNCaP (PSMA+) tumors 1, 24, and 48 h after tail vein injection of the indicated doses of DUPA-NIR (left) and gross images of excised LNCaP tumors and whole organs visualized for NIR signal after the last time points (right) (n = 3).