({5-[4,6-Di(aziridin-1-yl)-1,3,5-triazin-2-yl]amino}-2,2-dimethyl-1,3-dioxan-5-yl)-methyl 2-(5-phenyl-2H-tetrazol-2-yl)acetate was synthesized and characterized. The interaction of the obtained tetrazole-containing 2-amino-4,6-di(aziridin-1-yl)-1,3,5-triazine derivative with DNA was studied by UV spectrophotometry, circular dichroism spectroscopy, and isothermal calorimetry. The values of binding constants (9.65·10⁸ L mol⁻¹, UV spectrophotometry; 4.08·10⁸ L mol⁻¹, isothermal calorimetry) of the 1,3,5-triazine derivative to DNA attests to efficient binding and formation of stable associates with the biopolymer. The addition of the tetrazole-containing 1,3,5-triazine derivative to a DNA solution has virtually no effect on the DNA melting point. The tetrazole-containing 1,3,5-triazine derivative exhibits a cytostatic effect on SK-HEP-1 human hepatic adenocarcinoma cells (half-maximal inhibitory concentration IC₅₀ 22.2 mmol L⁻¹) and T98G human glioblastoma cells (IC₅₀ 44.9 mmol L⁻¹).