PR-104 是一种选择性缺氧激活的 DNA 交联剂，可用于多种异种肿瘤模型的研究。PR-104 作为氮芥的前体药物，可有效地转化为亲脂性较强的二硝基苯甲酰胺芥菜醇 PR-104A。

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.

Solid

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

-80°C, protect from light, stored under nitrogen

[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.

In Vitro: DMSO : 100 mg/mL (172.63 mM; Need ultrasonic)H₂O : 31.25 mg/mL (53.95 mM; ultrasonic and warming and heat to 60°C)配制储备液