DOTA-tris(TBE)-amido-dPEG®4-TFP ester, product number 11155, contains a DOTA-tris(TBE) group combined with a short discrete polyethylene glycol (dPEG®) spacer and functionalized with 2,3,5,6-tetrafluorophenyl (TFP) ester. The dPEG® linker is 16 atoms (17.8 Å) long. The TFP ester reacts specifically and efficiently with amines. See, TFP Esters Have More Hydrolytic Stability and Greater Reactivity than NHS Esters to understand the advantages of TFP esters over N-hydroxysuccinimide (NHS) esters
Polyethylene glycol (PEG) is frequently used to impart water solubility and flexibility to molecules and to reduce or eliminate immunogenicity of molecules. In vivo, PEG increases the hydrodynamic volume of molecules to which it is conjugated, because each ethylene glycol unit in a PEG chain can interact with up to three molecules of water through hydrogen bonding. Renal clearance of PEGylated conjugates is decreased or eliminated by the increased hydrodynamic volume. Reduced renal clearance means that lower doses of therapeutic agents can be administered.
Large, disperse PEG (Đ > 1) often is used to obtain the benefits of PEGylation described above. However, research over the past several years has proven that large, disperse PEG is not always needed. Moreover, in many cases, large, disperse PEG may work against the intended goals by, for example, reducing ligand affinity for a receptor or inhibiting cell internalization. By contrast, Quanta BioDesign produces only single molecular weight (that is, discrete) PEG products (that is Đ = 1). Our smaller dPEG® products avoid problems associated with large PEGs, while their discrete nature simplifies analysis of the dPEG® product and of conjugates formed with the dPEG® product. To learn more about the advantages of our products, see What is dPEG®?. For answers to frequently asked questions, please click here.
The macrocycle 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is a highly popular, effective bifunctional chelator that is used in radiopharmaceutical applications that require trivalent isotopes of yttrium or lanthanides. This form of DOTA has the four acetate groups protected with tert-butyl esters (TBE). This intermediate DOTA form is not an effective chelator, but it is useful in situations where the DOTA needs to be incorporated into the molecule at an early stage of development. To learn more, read DOTA-tris(TBE) or DOTA-tris(acid)? Choose wisely.
If you need bulk product in a larger package size than our standard sizes, please contact us for a quote. Our commercial capabilities permit us to manufacture this product at any scale that you need.
Hermanson, G. T. Chapter 2, Functional Targets for Bioconjugation. Bioconjugate Techniques, 3rd edition. Academic Press: New York, 2013, 127-228, specifically pages 191-192, discussing iodoacetates and bromoacetates reacting with thiols. Click here now for a review of Greg’s book and a link to purchase it.
Hermanson, G. T. Chapter 12, Isotopic Labeling Techniques. Bioconjugate Techniques, 3rd edition. Academic Press: New York, 2013, 507-534, specifically pages 508-509, discussing DOTA.
Hermanson, G. T. Chapter 18, PEGylation and Synthetic Polymer Modification. Bioconjugate Techniques, 3rd edition. Academic Press: New York, 2013, 787-838.
De León-Rodríguez, L. M.; Kovacs, Z. The Synthesis and Chelation Chemistry of DOTA−Peptide Conjugates. Bioconjugate Chem.2008, 19(2), 391–402. https://doi.org/10.1021/bc700328s.
Mier, W.; Haberkorn, U.; Eisenhut, M. Synthesis and Isolation of Active Esters of DOTA. Journal of Labelled Compounds and Radiopharmaceuticals2001, 44 (S1), S814–S816. https://doi.org/10.1002/jlcr.25804401286.
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