| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 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 5000) 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 5000 provides long circulation and steric stabilization.
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| ln Vivo |
No in vivo activity for the PEG-lipid alone; folate-targeted liposomes prepared with DSPE-PEG-Folate (MW 5000) demonstrate enhanced tumor accumulation and cellular uptake in FR-overexpressing tumor xenografts compared to non-targeted controls, leading to improved therapeutic efficacy of encapsulated payloads.
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| 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; cell-associated radioactivity is measured; IC50 is determined from displacement curves.
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| 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). Tumor accumulation is assessed by in vivo fluorescence imaging or by measuring payload concentration in tumor homogenates by LC-MS/MS.
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| ADME/Pharmacokinetics |
Not applicable; DSPE-PEG-Folate is a formulation component, not a therapeutic agent. PEG 5000 provides enhanced circulation half-life and reduced opsonization. Folate targeting does not alter the pharmacokinetics of the nanocarrier but improves tumor biodistribution.
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| Toxicity/Toxicokinetics |
No toxicity data for DSPE-PEG-Folate alone; PEGylated phospholipids have low inherent toxicity. Folate is a vitamin and has no toxicity. The compound is for research use only, not for human administration.
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| References |
[1]. Werner ME, et, al. Folate-targeted nanoparticle delivery of chemo- and radiotherapeutics for the treatment of ovarian cancer peritoneal metastasis. Biomaterials. 2011 Nov;32(33):8548-54.
[2]. Li Y, 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 Aug 19;7(32):17573-81. |
| Additional Infomation |
DSPE-PEG-Folate (MW 5000) 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.
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| Molecular Weight |
5000(Average)
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|---|---|
| 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 :~100 mg/mL
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (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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