Therapeutic efficacy of ²¹¹At-radiolabeled 2,6-diisopropylphenyl azide in mouse models of human lung cancer

Abstract

We developed 211At-radiolabeled 2,6-diisopropylphenyl azide (ADIPA) for targeted α-particle therapy. In the experiment using a mouse model, low-dose (70 kBq) administration of ADIPA effectively suppressed tumor growth without causing adverse effects.

Metallic radionuclide-labeled tetrameric 2,6-diisopropylphenyl azides for cancer treatment

“…1b, upper left) that selectively targets acrolein within cancer cells while remaining unreactive toward healthy cells. 11 Once inside cancer cells, ADIPA 3 undergoes the [3 + 2] cycloaddition reaction with acrolein, producing an α-diazocarbonyl derivative (Fig. 1b).…”