PR-104 sodium is a hypoxia-activated DNA cross-linking agent used in the research of tumor xenograft models. It functions as a nitrogen mustard pre-prodrug and efficiently transforms into the more lipophilic dinitrobenzamide mustards alcohol PR-104A.

PR-104 (sodium) demonstrates distinct biological activities in SiHa cells under different conditions and concentrations. At 80 μM for 1 hour, it more effectively suppresses radiation-induced DNA single-strand breaks under hypoxic conditions compared to aerobic ones. At a concentration of 100 μM for the same duration, it induces the phosphorylation of Ser139 on histone H2AX (gH2AX). Additionally, when administered at 0.266 mmol/kg for 18 hours, it exhibits activity against hypoxic cells post-irradiation. The efficacy of PR-104 (sodium) varies across cell lines, showing the lowest IC 50 value of 0.51 μmol/L in H460 cells and the highest at 7.3 μmol/L in PC3 prostate cells[1].

PR-104 (sodium), administered intravenously (i.v.) or intraperitoneally (i.p.) at a dosage of 0.56 mmol/kg within a 0-2 hour window, influences the plasma area under the curve in CD-1nu/nu mice, indicating its pharmacokinetic properties. At a lower dosage of 0.23 mmol/kg given i.p. over a period of 100 days in CD1-Foxn1nu mice, PR-104 (sodium) demonstrates antitumor activity, showcasing its potential therapeutic effects.