2941391-49-5

DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models[1]. DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

hCA IX: 0.25 nM (Kd)

[1] 1. Massière, et al. Preclinical Characterization of DPI-4452: A68Ga/177Lu Theranostic Ligand for Carbonic Anhydrase IX. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2024, 65(5), 761–767. DOI:10.2967/jnumed.123.266309