PR-104 sodium

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PR-104 sodium 

PR-104 (sodium) 是一种选择性低氧活化 DNA 交联剂,可用于多种肿瘤异种移植模型的研究。PR-104 (sodium) 作为氮芥前药物有效地转化为亲脂性更强的二硝基苯甲酰胺芥菜醇 PR-104A。

PR-104 sodium

PR-104 sodium Chemical Structure

CAS No. : 851627-80-0

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PR-104 sodium 的其他形式现货产品:

PR-104

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-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A[1].

体外研究
(In Vitro)

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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[1].

上海金畔生物科技有限公司 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.

Clinical Trial

分子量

601.25

Formula

C14H19BrN4NaO12PS

CAS 号

851627-80-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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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