| Size | Price | |
|---|---|---|
| 5mg | ||
| 10mg | ||
| Other Sizes |
| Targets |
Folate receptor (FRalpha/FRbeta), which is overexpressed on the surface of many cancer cells (e.g., ovarian, lung, breast). The folate moiety binds to FR, enabling receptor-mediated endocytosis of the nanocarrier.
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|---|---|
| ln Vitro |
DSPE-PEG-Folate (MW 2000) has no direct biological activity; it functions as a targeting excipient. The folate moiety specifically binds to folate receptors on cancer cells with high affinity (Kd in the low nanomolar range). PEG 2000 provides shorter spacer length compared to MW 5000, potentially affecting targeting efficiency.
|
| ln Vivo |
No in vivo activity for the PEG-lipid alone; folate-targeted liposomes prepared with DSPE-PEG-Folate (MW 2000) demonstrate enhanced tumor accumulation and cellular uptake in FR-overexpressing tumor xenografts. The MW 2000 version can be post-inserted into pre-formed liposomal bilayers to prepare folate-targeted formulations.
|
| Enzyme Assay |
Folate receptor binding affinity is assessed by competitive binding assay: FR-overexpressing cells (e.g., KB, HeLa) are incubated with radiolabeled folic acid ([3H]-folic acid) in the presence of increasing concentrations of DSPE-PEG-Folate (MW 2000); cell-associated radioactivity is measured; IC50 is determined from displacement curves.
|
| Cell Assay |
FR-overexpressing cancer cells (KB, HeLa, SKOV3) are incubated with folate-targeted liposomes containing fluorescent dye (e.g., DiD) or encapsulated payload at 37degC for 1-4 h; cellular uptake is assessed by flow cytometry or confocal microscopy; free folate (1 mM) is added as a competitor to confirm receptor-specific uptake.
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| Animal Protocol |
Mice bearing FR-overexpressing tumor xenografts (e.g., KB, HeLa, SKOV3) receive folate-targeted liposomes encapsulating therapeutic payload (doxorubicin, paclitaxel, or siRNA) or fluorescent dye via intravenous injection (0.5-5 mg lipid/kg). Formulations are prepared by post-insertion of DSPE-PEG-Folate (MW 2000) into pre-formed liposomes. Tumor accumulation is assessed by fluorescence imaging or LC-MS/MS.
|
| ADME/Pharmacokinetics |
Not applicable; DSPE-PEG-Folate is a formulation component, not a therapeutic agent. PEG 2000 provides circulation half-life extension and reduced opsonization, though with slightly shorter circulation time than PEG 5000. Folate targeting improves tumor biodistribution.
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| Toxicity/Toxicokinetics |
No toxicity data for DSPE-PEG-Folate (MW 2000) alone; PEGylated phospholipids have low inherent toxicity. Folate is a vitamin with no toxicity. The compound is for research use only, not for human administration.
|
| References |
[1]. Li Y, Lin J, Yang X, et al. Self-Assembled Nanoparticles Based on Amphiphilic Anticancer Drug-Phospholipid Complex for Targeted Drug Delivery and Intracellular Dual-Controlled Release. ACS Appl Mater Interfaces. 2015;7(32):17573-17581.
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| Additional Infomation |
DSPE-PEG-Folate (MW 2000) is a research-grade formulation excipient for targeted drug delivery to folate receptor-overexpressing tumors. It is not a drug and has no clinical trial or marketing approval status. For research use only.
|
| Molecular Weight |
2000 (Average)
|
|---|---|
| Appearance |
Typically exists as solid at room temperature
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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
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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.
Products are for research use only; We do not sell to patients
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