Description
PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.In VitroPR-104 (80 µM; 1 hour; SiHa cells) shows greater suppression of radiation-induced DNA single-strand breaks under hypoxic than aerobic conditions. PR-104 (100 µM; 1 hour; SiHa cells) results in phosphorylation of Ser139 of histone H2AX (gH2AX). PR-104 (0.266 mmol/kg; 18 h; SiHa cells) shows activity against hypoxic cells after irradiation. PR-104 varies in potency between cell lines, with the lowest IC 50 (0.51 µmol/L) in H460 cells and highest (7.3 µmol/L) in PC3 prostate cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoPR-104 (0.56 mmol/kg; i.v. or i.p.; 0~2 hours) makes the plasma area under the curve. PR-104 (0.23 mmol/kg; i.p.; 100 days) shows antitumor activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CD-1nu/nu mice Dosage: 0.56 mmol/kg (Pharmacokinetics Analysis) Administration: I.v. or i.p. Result: The plasma area under the curve. Animal Model: CD1-Foxn1nu mice Dosage: 0.23 mmol/kg Administration: I.p. Result: Showed antitumor activity.Form:Solid