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PR-104 sodium

Catalog No. T40947 CAS 851627-80-0

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.

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PR-104 sodium, CAS 851627-80-0

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Description	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.
In vitro	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].
In vivo	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.

Molecular Weight	602.26
Formula	C14H20BrN4NaO12PS
CAS No.	851627-80-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Patterson AV, et al. Mechanism of action and preclinical antitumor activity of the novel hypoxia-activated DNA cross-linking agent PR-104. Clin Cancer Res. 2007;13(13):3922-3932.

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Keywords

PR-104 sodium 851627-80-0 PR104 sodium PR 104 sodium inhibitor inhibit

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