| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary target of DSPE-PEG-Folate is the folate receptor (FR), particularly the folate receptor alpha (FRα) isoform, which is highly overexpressed on the surface of various cancer cells while being minimally expressed in normal tissues. The folic acid moiety of the molecule binds to the folate receptor with high affinity (Kd ~ 0.1-1 nM), enabling active targeting of drug delivery systems to FR-positive tumors. This receptor-mediated targeting enhances the selective uptake of nanoparticles into cancer cells via endocytosis, improving the therapeutic index of encapsulated drugs. The folate receptor is a validated target for cancer therapy, and DSPE-PEG-Folate is widely used in nanomedicine research to develop actively targeted drug delivery systems.
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| ln Vitro |
DSPE-PEG-Folate itself does not possess intrinsic cytotoxic activity; its biological activity is derived from its ability to functionalize drug delivery systems for targeted cancer therapy. In vitro, DSPE-PEG-Folate is incorporated into nanoparticles loaded with chemotherapeutic drugs, imaging agents, or nucleic acids. These folate-functionalized nanoparticles are then tested on folate receptor-overexpressing cancer cell lines. Studies demonstrate that these nanoparticles are primarily taken up via folate receptor-mediated endocytosis, leading to enhanced intracellular drug accumulation and improved cytotoxicity compared to non-targeted formulations. For example, folate-targeted nanoparticles have been shown to deliver chemotherapeutics and radiotherapeutics effectively to ovarian cancer cells.
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| ln Vivo |
DSPE-PEG-Folate-based formulations have been evaluated in vivo for their ability to enhance tumor targeting and improve therapeutic outcomes. When incorporated into nanoparticles, DSPE-PEG-Folate enables active tumor targeting through the folate receptor. In preclinical studies, folate-targeted nanoparticles have demonstrated increased accumulation in tumors, leading to improved antitumor efficacy and reduced systemic toxicity compared to non-targeted counterparts. For example, folate-targeted nanoparticles have been used for the delivery of chemo- and radiotherapeutics in models of ovarian cancer peritoneal metastasis, showing enhanced drug delivery and prolonged survival. The PEG component also prolongs circulation time by reducing clearance by the reticuloendothelial system.
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| Enzyme Assay |
DSPE-PEG-Folate is a functionalized lipid that does not directly bind to enzymes or receptors in cell-free systems; rather, its binding activity is assessed through the nanoparticles it forms. In vitro binding assays typically involve incubating folate-functionalized nanoparticles (e.g., fluorescently labeled liposomes) with folate receptor-overexpressing cancer cells. Binding is quantified using flow cytometry or fluorescence microscopy, with excess free folate used as a competitor to confirm receptor specificity. Surface plasmon resonance (SPR) or ELISA-based assays can also be used to measure the binding affinity of folate-functionalized nanoparticles to recombinant folate receptor protein.
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| Cell Assay |
Cellular assays for DSPE-PEG-Folate-based nanoparticles involve treating folate receptor-positive cancer cell lines (e.g., KB, HeLa, MCF-7, OVCAR-3) with drug-loaded or fluorescently labeled formulations. Cells are incubated with the nanoparticles for various time points, and cellular uptake is assessed by flow cytometry or confocal microscopy. The nanoparticles are shown to enter cells primarily via folate receptor-mediated endocytosis, with the drug payload accumulating in the cytoplasm and nucleus. Cytotoxicity is evaluated using MTT or similar assays to determine the enhanced killing effect of targeted versus non-targeted nanoparticles. Competition assays with excess free folate confirm the specificity of receptor-mediated uptake.
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| Animal Protocol |
In vivo efficacy of DSPE-PEG-Folate-based formulations is evaluated in xenograft mouse models bearing folate receptor-positive tumors. The nanoparticles, typically loaded with chemotherapeutic drugs or imaging agents, are administered intravenously. Tumor accumulation and biodistribution are assessed using fluorescence imaging, radiolabeling, or tissue analysis. Therapeutic efficacy is evaluated by measuring tumor growth inhibition, survival, and toxicity. For example, folate-targeted nanoparticles have been shown to significantly improve the delivery of chemo- and radiotherapeutics to ovarian cancer peritoneal metastases, leading to enhanced antitumor efficacy and prolonged survival compared to non-targeted formulations.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of DSPE-PEG-Folate are primarily determined by the nanoparticles or liposomes it is incorporated into. The PEG component (MW 3350) provides steric stabilization, reducing opsonization and extending circulation half-life by evading clearance by the mononuclear phagocyte system. The folate targeting moiety enhances the accumulation of nanoparticles at tumor sites by facilitating binding to folate receptors overexpressed on cancer cells. Studies have shown that folate-targeted nanoparticles exhibit prolonged circulation times and increased tumor uptake compared to non-targeted formulations. The DSPE lipid anchor integrates into the lipid bilayer, ensuring stable incorporation of the PEG-folate conjugate into the nanoparticle structure.
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| Toxicity/Toxicokinetics |
DSPE-PEG-Folate is a research-grade reagent used for the development of targeted drug delivery systems and is not intended for therapeutic use as a standalone compound. As such, comprehensive toxicity data specific to DSPE-PEG-Folate is limited. However, its components (DSPE, PEG, and folate) are generally considered biocompatible. DSPE is a phospholipid commonly used in FDA-approved liposomal formulations, PEG is widely used in pharmaceuticals to reduce immunogenicity and prolong circulation, and folate is a vitamin essential for human health. When incorporated into nanoparticles, DSPE-PEG-Folate-based formulations have been shown to be well-tolerated in preclinical studies, with the primary safety considerations related to the encapsulated drug payload rather than the lipid carrier itself.
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| References | |
| Additional Infomation |
DSPE-PEG-Folate is a widely used reagent in nanomedicine for the development of actively targeted drug delivery systems. Its folate moiety enables binding to folate receptors overexpressed on many cancer cells, facilitating receptor-mediated endocytosis and enhancing cellular uptake. This targeting strategy improves the therapeutic index of encapsulated drugs by increasing tumor accumulation and reducing systemic toxicity. DSPE-PEG-Folate is commonly used in the formulation of liposomes, lipid nanoparticles, and polymeric nanoparticles for the delivery of chemotherapeutics, nucleic acids, and imaging agents. It has been extensively studied in preclinical models of ovarian cancer, breast cancer, and other folate receptor-positive malignancies.
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| Molecular Formula |
(C2H4O)NC63H104N9O15P.2H3N
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| Molecular Weight |
1336.64(n=1)
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| Exact Mass |
1318.791
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| CAS # |
1236288-25-7
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| PubChem CID |
156593841
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| Appearance |
Yellow to brown solid powder
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
60
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| Heavy Atom Count |
92
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| Complexity |
2250
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(=NC(=O)C2C(NC=C(CNC3=CC=C(C=C3)C(NC(C(=O)O)CCC(NCCOC{-}CO{+n}C(=O)NCCOP(=O)(O)OCC(OC(CCCCCCCCCCCCCCCCC)=O)COC(=O)CCCCCCCCCCCCCCCCC)=O)=O)N=2)=N1)N.N.N
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| InChi Key |
WXIKCKLNMQSVPC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C65H108N9O16P.H3N/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-57(76)87-49-54(90-58(77)34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2)50-89-91(83,84)88-44-42-68-65(82)86-46-45-85-43-41-67-56(75)40-39-55(63(80)81)72-61(78)51-35-37-52(38-36-51)69-47-53-48-70-60-59(71-53)62(79)74-64(66)73-60;/h35-38,48,54-55,59,69H,3-34,39-47,49-50H2,1-2H3,(H,67,75)(H,68,82)(H,72,78)(H,80,81)(H,83,84)(H2,66,74,79);1H3
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| Chemical Name |
azane;5-[2-[2-[2-[2,3-di(octadecanoyloxy)propoxy-hydroxyphosphoryl]oxyethylcarbamoyloxy]ethoxy]ethylamino]-2-[[4-[(2-imino-4-oxo-4aH-pteridin-6-yl)methylamino]benzoyl]amino]-5-oxopentanoic acid
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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) |
DMSO: 50 mg/mL (14.71 mM)
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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.) |
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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