A prodrug of imidazotetrazine alkylating agent with antineoplastic property. Mitozolomide undergoes ring opening upon the nucleophilic attack at C-4 by an activated molecule of water within the major groove of DNA. The resulting bioactive mono-alkyltriazene species are capable of alkylating nucleophilic residues in the immediate vicinity such as N-7 and/or O-6 sites of guanine, thereby causes intra- or inter-stranded DNA cross-links and trigger apoptosis.