Figure 7.

Results from the blocking assay. The blocking effect of non-radiolabeled Tz was calculated as the change in tumor uptake of [¹¹¹In]1 22 h p.i. (A) General scheme of the blocking assay. First, tumor-bearing mice were administrated with CC49-TCO, 72 h before injection of a nonradioactive Tz. After 1 h, [¹¹¹In]1 was injected, and ex vivo biodistribution was performed 22 h p.i. to determine the blocking effect of the non-radiolabeled ¹⁹F-Tz. The uptake was normalized to a group of animals (control) in which no blocking was performed. (B) Structural Tz scaffolds. (C,D) Correlation of clogD_7.4 and blocking effect for Tz derivatives with alike IEDDA reactivity. (E) Statistical analysis of the correlation between blocking and tumor uptake for the different groups of Tz. Pearson’s correlation coefficient (r) describes the fit between the clogD_7.4 and blocking effect. Modified with permission from ACS. Copyright © 2021, American Chemical Society.