851627-80-0
851627-80-0 structure
- Name: PR-104 sodium
- Chemical Name: Sodium 2-({2-[(2-bromoethyl){2-[(methylsulfonyl)oxy]ethyl}amino]- 3,5-dinitrobenzoyl}amino)ethyl hydrogen phosphate
- CAS Number: 851627-80-0
- Molecular Formula: C14H19BrN4NaO12PS
- Molecular Weight: 601.25300
- Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA Alkylator/Crosslinker
- Create Date: 2016-05-18 07:21:54
- Modify Date: 2024-01-10 16:55:03
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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].
| Name | Sodium 2-({2-[(2-bromoethyl){2-[(methylsulfonyl)oxy]ethyl}amino]- 3,5-dinitrobenzoyl}amino)ethyl hydrogen phosphate |
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| Description | 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]. |
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| Related Catalog | |
| 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]. |
| 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]. 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 |
| Molecular Formula | C14H19BrN4NaO12PS |
|---|---|
| Molecular Weight | 601.25300 |
| Exact Mass | 599.95400 |
| PSA | 258.62000 |
| LogP | 3.09410 |