DSPE-PEG(5000) Folate | 880123

1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[folate(polyethylene glycol)-5000] (ammonium salt)





Chloroform/Methanol (9:1)


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Folate receptors are cellular surface markers for numerous solid tumors and myeloid leukemias.  Avanti now offers a derivative, DSPE-PEG-folate, which can be incorporated into liposomes as a targeting ligand.
Folate targeted drug delivery has emerged as an alternative therapy for the treatment and imaging of many cancers and inflammatory diseases. Due to its small molecular size and high binding affinity for cell surface folate receptors (FR), folate conjugates have the ability to deliver a variety of molecular complexes to pathologic cells without causing harm to normal tissues. Complexes that have been successfully delivered to FR expressing cells, to date, include protein toxins, immune stimulants, chemotherapeutic agents, liposomes, nanoparticles, and imaging agents. This review will summarize the applications of folic acid as a targeting ligand and highlight the various methods being developed for delivery of therapeutic and imaging agents to FR-expressing cells.
Hilgenbrink, A.R., Low, P.S. (2005). Folate Receptor-Mediated Drug Targeting: From Therapeutics to Diagnostics. Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 94:2135–2146.
According to the published synthetic protocol, the product will be 80-85% gamma conjugated and contain 15-20% of the other positional isomer. This does not seem to impact the functionality.
1 Years
CAS Number
CAS Registry Number is a Registered Trademark of the American Chemical Society
Molecular Weight
6226.473 (average MW due to polydispersity of PEG)
GIF Graphics File. 
GIF Graphics File. 
MDL Molfile. 
CDX File. 
Chiu, S.J., S. Liu, D. Perrotti, G. Marcucci, and R.J. Lee. (2006). Efficient delivery of a Bcl-2-specific antisense oligodeoxyribonucleotide (G3139) via transferrin receptor-targeted liposomes. J Control Release 112:199-207. [PubMed]Wu, J., Q. Liu, and R.J. Lee. (2006). A folate receptor-targeted liposomal formulation for paclitaxel. Int J Pharm 316:148-53. [PubMed]Shiokawa, T., Y. Hattori, K. Kawano, Y. Ohguchi, H. Kawakami, K. Toma, and Y. Maitani. (2005). Effect of polyethylene glycol linker chain length of folate-linked microemulsions loading aclacinomycin A on targeting ability and antitumor effect in vitro and in vivo. Clin Cancer Res 11:2018-25. [PubMed]Zhang, Y., L. Guo, R.W. Roeske, A.C. Antony, and H.N. Jayaram. (2004). Pteroyl-gamma-glutamate-cysteine synthesis and its application in folate receptor-mediated cancer cell targeting using folate-tethered liposomes. Anal Biochem 332:168-77. [PubMed]Gabizon, A., A.T. Horowitz, D. Goren, D. Tzemach, F. Mandelbaum-Shavit, M.M. Qazen, and S. Zalipsky. (1999). Targeting folate receptor with folate linked to extremities of poly(ethylene glycol)-grafted liposomes: in vitro studies. Bioconjug Chem 10:289-98. [PubMed]