Herein we present the preparation of two novel cyclam-based macrocycles (te1pyp and cb-te1pyp), bearing phosphonate-appended pyridine side arms for coordination copper(II) ions in context 64Cu PET imaging. The ligands have been prepared through conventional protection–alkylation sequences on cyclam, their properties thoroughly investigated. corresponding copper complexes fully characterized sol...

BACKGROUND In recent years, Copper-64 (T1/2 = 12.7 h) in the chemical form of copper dichloride ([64Cu]CuCl2) has been identified as a potential agent for PET imaging and radionuclide therapy targeting the human copper transporter 1, which is overexpressed in a variety of cancer cells. Limited human biodistribution and radiation dosimetry data is available for this tracer. The aim of this resea...

The purpose of this study was 2-fold: to determine the maximum tolerated dose (MTD) of 64Cu-bromoacetamidobenzyl- 1,4,8,11-tetraazacyclotetradecane-N,N',N'',N'''-tetraacetic acid (BAT)-2-iminothiolane (2IT)-monoclonal antibody (MAb) 1A3 in hamsters, and second, to determine the therapeutic efficacy of 64Cu-BAT-2IT-MAb 1A3 at various dose levels in hamsters with large (600 mg), 7-day-old GW39 hu...

UNLABELLED Bone diseases are often a result of increased numbers of osteoclasts, or bone-resorbing cells. Bone metastases are a significant cause of morbidity in many types of cancer. An imaging agent targeting osteoclasts, which are upregulated in osteolytic lesions, may facilitate earlier follow-up in patients with osteolytic or mixed bone metastases. Osteoclasts express high levels of alpha(...

Angiogenesis plays a key role in cancer progression and correlates with disease aggressiveness and poor clinical outcomes. Affinity ligands discovered by screening phage display random peptide libraries can be engineered to molecularly target tumor blood vessels for noninvasive imaging and early detection of tumor aggressiveness. In this study, we tested the ability of a phage-display-selected ...

pr81 is a monoclonal antibody that binds with high affinity to muc1 that over expressed on breast tumors. pr81 is considered a suitable targeting molecule that was radiolabeled using cu-64 for positron imaging studies. the monoclonal antibody was conjugated with dota moiety and after purification was evaluated for radiochemical purity, immunoreactivity, cell toxicity and structure integrity as ...

in the present study, aqueous solutions of some copper-complexing ligands were screened for their cytotoxicity using brine shrimp lethality test. among the ligands tested, diacetyl-bis(n4-methylthiosemicarbazones) (atsm) proved to be the most safe and non-toxic compound (2% lethality at 10 ppm), while pyruvaldehyde bis(n4-methyl)thiosemicarbazone (ptsm) was shown to possess low toxicity (7% let...

The 64Cu incorporation into fibroblast clones obtained from three obligate and three suspected Menkes disease heterozygotes was studied. For each obligate heterozygote, two clonal cell populations were observed, one with a Menkes phenotype and one with a normal phenotype, as predicted by the Lyon hypothesis. The cloning results suggested a heterozygous state in two of the suspected carriers. Th...