| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The azide group on DSPE-PEG 2000-N3 enables bioorthogonal click chemistry reactions, particularly copper-free strain-promoted azide-alkyne cycloaddition (SPAAC) with dibenzocyclooctyne (DBCO)-modified molecules. This allows for the conjugation of the lipid-PEG construct to various biomolecules including peptides, proteins, antibodies, and small molecules. The DSPE moiety anchors the construct into lipid bilayers, while the PEG chain provides steric stabilization and reduces non-specific interactions. This makes DSPE-PEG 2000-N3 a valuable tool for drug delivery and nanoparticle functionalization.
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| ln Vitro |
In vitro, DSPE-PEG 2000-N3 is used to functionalize liposomes and lipid nanoparticles (LNPs) for targeted drug delivery. The azide group enables the attachment of targeting ligands via click chemistry, allowing for specific cell targeting. The PEG chain reduces protein adsorption and macrophage uptake, increasing particle circulation time. In cell culture studies, DSPE-PEG 2000-N3-functionalized nanoparticles show improved stability, reduced non-specific binding, and enhanced cellular uptake when conjugated to targeting moieties.
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| ln Vivo |
In vivo, DSPE-PEG 2000-N3-functionalized liposomes and LNPs exhibit prolonged circulation time due to the "stealth" properties of the PEG coating, which reduces recognition and clearance by the reticuloendothelial system. The azide group enables in vivo click chemistry for active targeting of lymph nodes or tumors. Studies have shown that DBCO-modified liposomes with azide targeting achieve enhanced therapeutic effects and prolonged survival in mouse models. This makes DSPE-PEG 2000-N3 a valuable tool for developing targeted drug delivery systems and cancer vaccines.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to DSPE-PEG 2000-N3, as it is not a receptor ligand but a functionalized lipid-PEG conjugate. However, click chemistry efficiency assays assess the reactivity of the azide group with DBCO or alkyne-containing molecules. These assays use fluorescently labeled DBCO probes and measure conjugation efficiency by fluorescence or gel electrophoresis. Particle characterization assays (dynamic light scattering, zeta potential) evaluate the physical properties of DSPE-PEG 2000-N3-containing nanoparticles. Protein adsorption studies measure the "stealth" properties of the PEG coating.
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| Cell Assay |
In vitro cellular assays for DSPE-PEG 2000-N3-functionalized nanoparticles are performed in cell lines to assess targeting, uptake, and efficacy. Cells are treated with nanoparticles containing DSPE-PEG 2000-N3 conjugated to targeting ligands or therapeutic payloads. Cellular uptake is measured by fluorescence microscopy or flow cytometry using labeled nanoparticles. Cytotoxicity is assessed by MTT or CellTiter-Glo assays. For vaccine applications, antigen presentation and T cell activation are evaluated in immune cell co-culture systems. These assays confirm the functionality of the azide-based conjugation strategy.
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| Animal Protocol |
In vivo animal studies with DSPE-PEG 2000-N3 are conducted in mouse models for drug delivery and vaccine applications. The compound is incorporated into liposomes or LNPs containing therapeutic agents or vaccine components. Animals receive the formulations via intravenous or subcutaneous injection. Biodistribution is assessed by imaging or tissue analysis using labeled nanoparticles. Efficacy is evaluated by measuring tumor growth inhibition, immune response, or survival. These studies demonstrate the utility of DSPE-PEG 2000-N3 for targeted delivery and immunotherapy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DSPE-PEG 2000-N3 are determined by its incorporation into lipid-based nanoparticles. The PEG coating provides "stealth" properties that reduce opsonization and clearance by the reticuloendothelial system, prolonging circulation time. The compound's large molecular weight (~2816 g/mol) and amphiphilic nature limit its distribution as a free molecule. When incorporated into nanoparticles, the pharmacokinetics are governed by the particle size, surface properties, and route of administration. The azide group is stable in biological environments for click chemistry applications.
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| Toxicity/Toxicokinetics |
Toxicological data for DSPE-PEG 2000-N3 are limited, as it is a research reagent for drug delivery applications. The DSPE and PEG components are generally regarded as safe and biocompatible. The azide group is stable and does not release toxic byproducts under physiological conditions. When incorporated into nanoparticles, toxicity depends on the overall formulation including the payload and other components. Standard toxicology assessments would be required for clinical applications. The compound is for research use only.
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| References |
[1]. Senouwa Segla Koffi DossouDevelopment of a Cancer Vaccine Using In Vivo Click-Chemistry-Mediated Active Lymph Node Accumulation for Improved Immunotherapy. Adv Mater. 2021 May;33(20):e2006007.
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| Additional Infomation |
Cancer vaccines are a promising cancer treatment strategy due to their ability to induce potent immune responses and low systemic toxicity. Significant efforts have been devoted to improving the in vivo efficacy of cancer vaccines, with direct targeting of lymph nodes (LNs) being one of the most promising approaches. This paper develops an Active Lymph Node Accumulation System (ALAS) based on click chemistry. This system enhances the delivery efficiency of encapsulated antigens and adjuvants to lymph nodes by modifying the surface of lymphatic endothelial cells with azide groups to provide a target for dibenzocyclooctylene (DBCO)-modified liposomes. When loaded with OVA257-264 peptide and polyinosinic cytidine diphosphate (poly(I:C)), this formulation induces an enhanced CD8+ T cell response in vivo, significantly improving therapeutic efficacy and prolonging median survival in mice. Compared to treatment with DBCO-coupled liposomes (DL)-Ag/Ad without azide targeting, mice treated with the ALAS vaccine showed a 100% increase in 60-day survival. In conclusion, the results indicate that the novel ALAS approach is an effective strategy for delivering vaccine components to lymph nodes to enhance anti-tumor immunity. [1]
DSPE-PEG 2000-N3 is a functionalized phospholipid-PEG conjugate with an azide terminal group, used for PEG-biochemical conjugation and lipid-based drug carrier development. It enables click chemistry-mediated attachment of targeting ligands to liposomes and LNPs for targeted drug delivery and vaccine applications. The compound has been used in cancer vaccine development to improve lymph node accumulation and antitumor immunity. It is for research use only, not for human use. |
| Molecular Formula |
C132H264N5O54P
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|---|---|
| Molecular Weight |
2816.47
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| Appearance |
Typically exists as solids at room temperature
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| Chemical Name |
1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[azido(polyethylene glycol)-2000]
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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 | 0.3551 mL | 1.7753 mL | 3.5505 mL | |
| 5 mM | 0.0710 mL | 0.3551 mL | 0.7101 mL | |
| 10 mM | 0.0355 mL | 0.1775 mL | 0.3551 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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