Abstract
Antineoplastons (ANPs) are compounds that have antitumor activities. ANPA(10) was labeled with technetium-99m using stannous chloride as a reducing agent with the labeling yield of approximately 98% at pH 6. The conditions required to optimize the labeling yield were studied in details. The tumor binding specificity of the [Tc-99m]Tc-ANPA(10) radiotracer was evaluated. The uptake of [Tc-99m]Tc-ANPA(10) in ascitic fluid uptake was 10, 16, and 12.8% ID/g at 30, 60, and 120 min post injection. The preclinical biological evaluation of [Tc-99m]Tc-ANPA(10) complex in solid tumor bearing mice showed a high tumor uptake at 1 h post injection (11.2 +/- 0.30 % ID/g). The selective uptake of [Tc-99m]Tc-ANPA(10) in solid tumors and rapid clearance from nontarget organs make it promising for solid tumor imaging, but further clinical trials are required.