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编 号：F760705
分子式：C14H19BrN4NaO12PS
分子量：601.25
分子式：C14H19BrN4NaO12PS
分子量：601.25
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CAS No: 851627-80-0
产品详情
生物活性：
PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
体内研究：
PR-104 (sodium) (0.56 mmol/kg; i.v. or i.p.; 0~2 hours) makes the plasma area under the curve. PR-104 (sodium) (0.23 mmol/kg; i.p.; 100 days) shows antitumor activity.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.
体外研究：
PR-104 (sodium) (80 μM; 1 hour; SiHa cells) shows greater suppression of radiation-induced DNA single-strand breaks under hypoxic than aerobic conditions. PR-104 (sodium) (100 μM; 1 hour; SiHa cells) results in phosphorylation of Ser139 of histone H2AX (gH2AX). PR-104 (sodium) (0.266 mmol/kg; 18 h; SiHa cells) shows activity against hypoxic cells after irradiation. PR-104 (sodium) varies in potency between cell lines, with the lowest IC50 (0.51 μmol/L) in H460 cells and highest (7.3 μmol/L) in PC3 prostate cells.
PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
体内研究：
PR-104 (sodium) (0.56 mmol/kg; i.v. or i.p.; 0~2 hours) makes the plasma area under the curve. PR-104 (sodium) (0.23 mmol/kg; i.p.; 100 days) shows antitumor activity.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.
体外研究：
PR-104 (sodium) (80 μM; 1 hour; SiHa cells) shows greater suppression of radiation-induced DNA single-strand breaks under hypoxic than aerobic conditions. PR-104 (sodium) (100 μM; 1 hour; SiHa cells) results in phosphorylation of Ser139 of histone H2AX (gH2AX). PR-104 (sodium) (0.266 mmol/kg; 18 h; SiHa cells) shows activity against hypoxic cells after irradiation. PR-104 (sodium) varies in potency between cell lines, with the lowest IC50 (0.51 μmol/L) in H460 cells and highest (7.3 μmol/L) in PC3 prostate cells.
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