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Tissue Distribution of Copper-Labeled 3-Ethoxy-2-oxobutyraldehyde bis (Thiosemicarbazone) (Cu-64 KTS) in Mice and Rats: Concise Communication

University of Wisconsin Hospital, Madison
University of Wisconsin—Milwaukee, Milwaukee, Wisconsin

Correspondence: For reprints contact: L. M. Lieberman, Sect. of Nuclear Medicine, Univ. of Wisconsin Hospitals, Ctr. for Health Sciences, 600 Highland Ave., Madison, WI 53792.

ABSTRACT

The antitumor activity of, 3-ethoxy-2-oxobutyraldehyde bis (thiosemicarbazone) (KTS), is related to the presence of copper(II) ion. We have studied the tissue distribution of Cu-64-labeled KTS in rats and mice carrying transplanted tumors to evaluate whether the uptake of the radioactivity in the tumor is adequate to warrant further investigation of the tracer as a tumor-seeking agent in patients.

Four groups of three or four animals each were studied: (a) mice with fibrosarcoma; (b) mice with mammary adenocarcinoma; (c) rats with fibrosarcoma; and (d) rats with squamous cell carcinoma of the lung. The animals were killed at intervals of 0.25, 1, 4, 24, and 48 hr after i.v. injection of 1.6 x 10^–3 M Cu·KTS containing 3 to 18 µCi Cu-64. Blood, tumor, and six to ten additional tissues were counted for radioactivity.

The mouse fibrosarcoma concentrated Cu-64, reaching 15% of the administered dose/g at 48 hr after injection. This suggests that for tumor scanning, the 61.7-hr Cu-67 might be more suitable as a label for KTS than the 12.7-hr Cu-64.