| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
N(1),N(11)-Diethylnorspermine (DENSPM) is a potent inducer of the polyamine catabolic enzyme, spermidine/spermine N1-acetyltransferase. It is able to increase enzyme activity by 200-1000 fold.
| ln Vivo |
In mice containing DU-145 cell line xenografts, N1,N11-diethylnorspermine (40 mg/kg three times daily for two cycles every six days) dramatically inhibits tumor growth[1].
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| References |
[1]. Schipper RG, et al. Antitumor activity of the polyamine analog N(1), N(11)-diethylnorspermine against human prostate carcinoma cells. Prostate. 2000 Sep 1;44(4):313-21.
[2]. Holst CM, et al. Molecular mechanisms underlying N1, N11-diethylnorspermine-induced apoptosis in a human breast cancer cell line. Anticancer Drugs. 2008 Oct;19(9):871-83. [3]. Jiang R, et al. Activation of polyamine catabolism by N1,N11-diethylnorspermine leads to cell death in glioblastoma. Int J Oncol. 2007 Aug;31(2):431-40. |
| Additional Infomation |
DENSPM is n(1),N(11)-bis(ethyl)norspermine (DENSPM), a N-terminally alkylated tetraamine and polyamine mimetics, disrupts polyamine pool homeostasis by modulating the activities of the biosynthetic enzymes, ornithine decarboxylase (ODC), and S-adenosylmethionine decarboxylase (AdoMetDC).
Diethylnorspermine is a synthetic bis-ethyl analogue of spermine with potential antineoplastic activity. N(1),N(11)-bis(ethyl)norspermine (DENSPM), a N-terminally alkylated tetraamine and polyamine mimetics, disrupts polyamine pool homeostasis by modulating the activities of the biosynthetic enzymes, ornithine decarboxylase (ODC), and S-adenosylmethionine decarboxylase (AdoMetDC). This agent also reduces polyamine concentrations through the induction of the catabolic enzyme spermidine/spermine N1-acetyltransferase 1 (SSAT). Polyamines, an integral part of the DNA helix structure, play a critical role in cell division, differentiation and membrane function. Disruption of normal polyamine concentrations by DENSPM may lead to cell growth inhibition. Drug Indication Investigated for use/treatment in renal cell carcinoma, pancreatic cancer, melanoma, and lung cancer. |
| Molecular Formula |
C13H32N4
|
|---|---|
| Molecular Weight |
244.427
|
| Exact Mass |
388.169
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| CAS # |
121749-39-1
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| Related CAS # |
N1,N11-Diethylnorspermine tetrahydrochloride;156886-85-0
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| PubChem CID |
4282
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| Appearance |
Typically exists as solid at room temperature
|
| Density |
0.877 g/cm3
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| Boiling Point |
357.1ºC at 760 mmHg
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| Flash Point |
171.9ºC
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| Vapour Pressure |
2.79E-05mmHg at 25°C
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| Index of Refraction |
1.462
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| LogP |
5.326
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
17
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| Complexity |
117
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCNCCCNCCCNCCCNCC
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| InChi Key |
UMJJGDUYVQCBMC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H32N4/c1-3-14-8-5-10-16-12-7-13-17-11-6-9-15-4-2/h14-17H,3-13H2,1-2H3
|
| Chemical Name |
N-ethyl-N'-[3-[3-(ethylamino)propylamino]propyl]propane-1,3-diamine
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| Synonyms |
DE-333 De 333 N(1),N(11)-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 |
| 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 | 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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