[CAS NO. 851627-62-8] PR-104
PRODUCTS SPECIFICATIONS [851627-62-8]
DESCRIPTION [851627-62-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 579.27 |
| Molecular Formula | C14H20BrN4O12PS |
| SMILES | O=C(NCCOP(O)(O)=O)C1=CC([N+]([O-])=O)=CC([N+]([O-])=O)=C1N(CCBr)CCOS(=O)(C)=O |
Summary
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] .
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 IC 50 (0.51 μmol/L) in H460 cells and highest (7.3 μmol/L) in PC3 prostate cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE 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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00862134 | Proacta, Incorporated |
Non-Small Cell Lung Cancer
|
March 2009 | Phase 2 |
| NCT00862082 | Proacta, Incorporated |
Hepatocellular Carcinoma
|
March 2009 | Phase 1|Phase 2 |
| NCT00544674 | Proacta, Incorporated |
Lung Cancer
|
August 2007 | Phase 2 |
| NCT00616213 | Proacta, Incorporated |
Unspecified Adult Solid Tumor, Protocol Specific
|
February 2008 | Phase 1 |
| NCT01037556 | Proacta, Incorporated |
Acute Myelogenous Leukemia|Acute Lymphocytic Leukemia
|
January 2010 | Phase 1|Phase 2 |
| NCT00349167 | Proacta, Incorporated|National Cancer Institute (NCI) |
Unspecified Adult Solid Tumor, Protocol Specific
|
December 2005 | Phase 1 |
| NCT01358227 | Proacta, Incorporated |
Unspecified Adult Solid Tumor, Protocol Specific
|
December 2006 | Phase 1 |
| NCT00459836 | Proacta, Incorporated |
Unspecified Adult Solid Tumor, Protocol Specific
|
February 2007 | Phase 1 |
Appearance
Solid
Shipping
Shipping with dry ice.
Storage
-80°C, protect from light, stored under nitrogen
Solvent & Solubility
DMSO : 100 mg/mL ( 172.63 mM ; Need ultrasonic)
H 2 O : 31.25 mg/mL ( 53.95 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7263 mL | 8.6316 mL | 17.2631 mL |
| 5 mM | 0.3453 mL | 1.7263 mL | 3.4526 mL |
| 10 mM | 0.1726 mL | 0.8632 mL | 1.7263 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (8.63 mM); Clear solution
Synonyms