biostudies-literatureYang XNCI NIH HHS33733-42https://www.ebi.ac.uk/biostudies/studies/S-EPMC4741798biostudies-literatureUnknown6(32)We developed a new scaffold for radionuclide-based imaging and therapy of clear cell renal cell carcinoma (ccRCC) targeting carbonic anhydrase IX (CAIX). Compound XYIMSR-01, a DOTA-conjugated, bivalent, low-molecular-weight ligand, has two moieties that target two separate sites on CAIX, imparting high affinity. We synthesized [111In]XYIMSR-01 in 73.8-75.8% (n = 3) yield with specific radioactivities ranging from 118 - 1,021 GBq/μmol (3,200-27,600 Ci/mmol). Single photon emission computed tomography of [111In]XYIMSR-01 in immunocompromised mice bearing CAIX-expressing SK-RC-52 tumors revealed radiotracer uptake in tumor as early as 1 h post-injection. Biodistribution studies demonstrated 26% injected dose per gram of radioactivity within tumor at 1 h. Tumor-to-blood, muscle and kidney ratiOncotargetImaging of carbonic anhydrase IX with an 111In-labeled dual-motif inhibitor.PMC4741798P30 CA006973R01 CA134675R03 CA197470CA197470CA134675Minn IKoo SMPomper MGSysa-Shah PGorin MAAllaf MEMease RCYang XBrummet MLee HSNimmagadda SRowe SPBanerjee SRfalseImaging of carbonic anhydrase IX with an 111In-labeled dual-motif inhibitor.We developed a new scaffold for radionuclide-based imaging and therapy of clear cell renal cell carcinoma (ccRCC) targeting carbonic anhydrase IX (CAIX). Compound XYIMSR-01, a DOTA-conjugated, bivalent, low-molecular-weight ligand, has two moieties that target two separate sites on CAIX, imparting high affinity. We synthesized [111In]XYIMSR-01 in 73.8-75.8% (n = 3) yield with specific radioactivities ranging from 118 - 1,021 GBq/μmol (3,200-27,600 Ci/mmol). Single photon emission computed tomography of [111In]XYIMSR-01 in immunocompromised mice bearing CAIX-expressing SK-RC-52 tumors revealed radiotracer uptake in tumor as early as 1 h post-injection. Biodistribution studies demonstrated 26% injected dose per gram of radioactivity within tumor at 1 h. Tumor-to-blood, muscle and kidney rati2015-01-01T00:00:00Z2015 Oct2026-05-29T20:23:16.216Z2019-03-27T02:08:26ZS-EPMC47417982641887610.18632/oncotarget.5254