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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
In comparison to aerobic settings, PR-104 (sodium) (80 μM; 1 hour; SiHa cells) exhibits a higher inhibition of radiation-induced DNA single-strand breaks under hypoxic conditions. Ser139 of histone H2AX (gH2AX) is phosphorylated in response to PR-104 (sodium) (100 μM; 1 hour; SiHa cells). PR-104 (sodium) (0.266 mmol/kg; 18 h; SiHa cells) exhibits anti-hypoxic action following radiation treatment. PR-104 (sodium) has different potencies in different cell lines; H460 cells have the lowest IC50 (0.51 μmol/L) and PC3 prostate cells have the highest (7.3 μmol/L)[1].
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ln Vivo |
The plasma area under the curve is made by PR-104 (sodium) (0.56 mmol/kg; iv or ip; 0~2 hours). Antitumor efficacy is demonstrated by PR-104 (sodium) (0.23 mmol/kg; ip; 100 days)[1].
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Animal Protocol |
Animal/Disease Models: CD-1nu/nu (nude) mice
Doses: 0.56 mmol/kg (pharmacokinetic/PKs Analysis) Route of Administration: Iv or ip Experimental Results: The plasma area under the curve. Animal/Disease Models: CD1-Foxn1nu (nude) mice Doses: 0.23 mmol/kg Route of Administration: Ip Experimental Results: demonstrated 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.
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Molecular Formula |
C14H19BRN4NAO12PS
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Molecular Weight |
601.25
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Exact Mass |
600.96
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CAS # |
851627-80-0
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Related CAS # |
PR-104;851627-62-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CS(=O)(=O)OCCN(CCBr)C1=C(C=C(C=C1[N+](=O)[O-])[N+](=O)[O-])C(=O)NCCOP(=O)(O)O.[Na]
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InChi Key |
WQCXXHGWABIMCR-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H20BrN4O12PS.Na/c1-33(28,29)31-7-5-17(4-2-15)13-11(14(20)16-3-6-30-32(25,26)27)8-10(18(21)22)9-12(13)19(23)24;/h8-9H,2-7H2,1H3,(H,16,20)(H2,25,26,27);
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Synonyms |
PR-104 sodium
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6632 mL | 8.3160 mL | 16.6320 mL | |
5 mM | 0.3326 mL | 1.6632 mL | 3.3264 mL | |
10 mM | 0.1663 mL | 0.8316 mL | 1.6632 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Hypoxia-selective cytotoxicity of PR-104A against human tumor cell lines in vitro. Clin Cancer Res . 2007 Jul 1;13(13):3922-32. td> |
Metabolites in stirred SiHa cell suspensions incubated with PR-104A under hypoxia. Clin Cancer Res . 2007 Jul 1;13(13):3922-32. td> |
Hypoxia-selective DNA damage by PR-104A. Clin Cancer Res . 2007 Jul 1;13(13):3922-32. td> |
Pharmacokinetics of PR-104 in CD-1 nu/nu mice. Clin Cancer Res . 2007 Jul 1;13(13):3922-32. td> |