851627-62-8

851627-62-8 structure

Name: PR-104
Chemical Name: 2-[N-(2-bromoethyl)-2,4-dinitro-6-(2-phosphonooxyethylcarbamoyl)anilino]ethyl methanesulfonate
CAS Number: 851627-62-8
Molecular Formula: C₁₄H₂₀BrN₄O₁₂PS
Molecular Weight: 579.27100
Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA Alkylator/Crosslinker
Create Date: 2017-02-08 00:34:12
Modify Date: 2024-01-18 18:46:06
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-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A[1].

Name	2-[N-(2-bromoethyl)-2,4-dinitro-6-(2-phosphonooxyethylcarbamoyl)anilino]ethyl methanesulfonate
Synonyms	2-((2-Bromoethyl)(2,4-dinitro-6-((2-(phosphonooxy)ethyl)carbamoyl)phenyl)amino)ethyl methanesulfonate PR104 UNII-V16D2ZT7DT

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-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> DNA Alkylator/Crosslinker
In Vitro	PR-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 IC50 (0.51 μmol/L) in H460 cells and highest (7.3 μmol/L) in PC3 prostate cells[1].
In Vivo	PR-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[1]. 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.
References	[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.