| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 1g | |||
| Other Sizes |
| Targets |
Diethylnorspermine targets spermidine/spermine N1-acetyltransferase (SSAT), a key enzyme in polyamine catabolism. It acts as a potent inducer of SSAT, increasing its expression and activity. By inducing SSAT, diethylnorspermine depletes intracellular polyamine pools, which are essential for cell proliferation. This mechanism underlies its anticancer activity.
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|---|---|
| ln Vitro |
In vitro, diethylnorspermine inhibits the proliferation of PC3, TSU-pr1, DU145, and JCA-1 prostate cancer cells with IC50s of 65, 62, 3, and 21 µM, respectively. It effectively induces SSAT mRNA and stabilizes SSAT enzyme activity. These in vitro activities confirm its profile as an SSAT inducer and an antiproliferative agent against cancer cells.
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| ln Vivo |
In vivo, diethylnorspermine has been studied as an anticancer agent. However, specific details of in vivo efficacy studies, such as the animal models used and the dosing regimens, are not extensively detailed in the available literature. The compound is a research tool for studying polyamine metabolism and cancer therapy.
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| Enzyme Assay |
The in vitro enzyme assay for diethylnorspermine measures its ability to induce SSAT activity. These assays typically use cell lysates or purified enzyme and measure the acetylation of spermidine or spermine. The compound's potency as an SSAT inducer is determined by measuring the increase in SSAT activity. Its effects on SSAT mRNA expression can also be assessed.
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| Cell Assay |
In vitro cellular assays for diethylnorspermine assess its antiproliferative effects and its ability to induce SSAT. Prostate cancer cell lines (PC3, TSU-pr1, DU145, JCA-1) are treated with various concentrations of the compound, and cell proliferation is measured. SSAT activity and mRNA levels are measured to confirm the compound's mechanism of action.
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| Animal Protocol |
In vivo animal studies for diethylnorspermine have been conducted in models of prostate cancer to assess its antitumor efficacy. However, specific details of these studies are not extensively detailed in the available literature. The compound is primarily used as a research tool for studying polyamine metabolism and cancer.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for diethylnorspermine 4HCl are not extensively detailed in the available literature. As a polyamine analogue, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as oral bioavailability, half-life, and distribution are not provided. The compound is primarily used in research settings.
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| Toxicity/Toxicokinetics |
Specific toxicity data for diethylnorspermine 4HCl are not extensively detailed in the available literature. As an anticancer polyamine analogue, its toxicity profile is likely related to its mechanism of action. However, preclinical toxicology studies would be required to assess its safety margin. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Diethylnorspermine 4HCl is the tetrahydrochloride salt of N1,N11-diethylnorspermine (DENSPM), a potent inducer of spermidine/spermine N1-acetyltransferase (SSAT). It is an anticancer polyamine that inhibits the proliferation of prostate cancer cells. It effectively induces SSAT mRNA and stabilizes SSAT enzyme activity. It is a research compound for studying polyamine metabolism and cancer therapy and is not approved for clinical use.
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| Molecular Formula |
C13H32N4
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|---|---|
| Molecular Weight |
244.43
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| Exact Mass |
388.169
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| CAS # |
156886-85-0
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| Related CAS # |
N1,N11-Diethylnorspermine;121749-39-1
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| PubChem CID |
11501988
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
21
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| Complexity |
117
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LAWBSOKBIROCQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H32N4.4ClH/c1-3-14-8-5-10-16-12-7-13-17-11-6-9-15-4-2;;;;/h14-17H,3-13H2,1-2H3;4*1H
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| Chemical Name |
N-ethyl-N'-[3-[3-(ethylamino)propylamino]propyl]propane-1,3-diamine;tetrahydrochloride
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| Synonyms |
BE-333 HCl BE333 HClBE 333 HCl DE333 BE 3-3-3 BE-333 tetrahydrochloride DE-333DE 333 BE333BE 333 BE-333N(1),N(11)-DiethylnorspermineDENSPMBENSPM N1,N11-Bis(ethyl)norspermineDiethyl-norspermine N1,N11-Diethylnorspermine
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~33.33 mg/mL (~85.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (256.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0912 mL | 20.4558 mL | 40.9115 mL | |
| 5 mM | 0.8182 mL | 4.0912 mL | 8.1823 mL | |
| 10 mM | 0.4091 mL | 2.0456 mL | 4.0912 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.
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