Artstrip world

Chelator Screening and Synthesis Service

The Chelator in RDC (Radionuclide Drug Conjugate) is used to link the radionuclide and the targeting molecule in order to integrate the targeting and effectiveness of RDC. A number of chelators are now applied in the conjugation process.

Overview of Chelators

Chelation is a type of bonding of metal ions to other molecules, forming multiple bonded between the ligand and the central metal atom. The coordination atoms in chelators are oxygen and nitrogen as the most common, followed by sulfur, as well as phosphorus, and arsenic. Before radionuclide can be used for clinical applications, there is a need to seclude the free radionuclide from aqueous solution by chelators to prevent the trans-chelation and hydrolysis processes. As a result, the chelator is widely applied in novel conjugated drugs, especially essential for RDC, which connects the radionuclide and the delivery part.

Examples of Chelators in RDC

We have more than 10 types of chelators. The chelating agents shown below are a representative portion of our chelating agent library.

    • DOTA (1,4,7,10-tetraazacyclododecane-N,N’,N”,N”’-tetraacetic acid)
      DOTA, an octadentate ligand, has a high-affinity chelating agent for di- and trivalent cations, binding the metal ions through four amine and four carboxylate groups.

Chemical structure diagram of DOTA chelated with radionuclide.Fig.1 Chemical structure diagram of DOTA chelated with radionuclide.

    • DTPA (2,2′,2”,2”’-{[(Carboxymethyl)azanediyl] bis(ethane-2,1-diylnitrilo)} tetraacetic acid)
      DTPA, an aminopolycarboxylic acid, consisting of a diethylenetriamine backbone with five carboxymethyl groups, can form up to eight bonds when wrapping around a metal ion.

Chemical structure diagram of DPTA chelated with radionuclide.Fig.2 Chemical structure diagram of DTPA chelated with radionuclide.

    • TETA (N1, N1′-(Ethane-1,2-diyl) di(ethane-1,2-diamine))
      TETA is a tetradentate ligand, commonly used as a chelating agent to bind and remove excess copper ion in the patients with Wilson’s disease. 

Chemical structure diagram of TETA chelated with radionuclide.Fig.3 Chemical structure diagram of TETA chelated with radionuclide.

    • NOTA (1,4,7-Triazacyclononane-1,4,7-triacetic acid)
      NOTA, a hexavalent ligand, is an essential bi-functional chelator utilized for the linkage of metal ions in radiopharmaceutical applications.

Chemical structure diagram of NOTA chelated with radionuclideFig.4 Chemical structure diagram of NOTA chelated with radionuclide.

    • HBED ((N, N’-di(2-hydroxybenzyl) ethylenediamine-N, N’-diacetic acid))
      HBED, a hexavalent ligand, can chelate with iron ions to inhibit iron-mediated production of hydroxyl radicals in organisms.

Chemical structure diagram of HBED chelated with radionuclide.Fig.5 Chemical structure diagram of HBED chelated with radionuclide.

    • NETA ({4-[2-(bis-carboxy-methylamino)-5-(4-nitrophenyl) pentyl]-7-carbo-xymethyl- [1,4,7] triazanonan-1-yl} acetic acid)
      NETA, as a bi-functional chelator utilized in targeted radiotherapy binding with Y-90, Lu-177, Bi-212, and Bi-213, can rapidly form a stable complex with the radioisotopes by the chelating backbone.

Fig.6 Chemical structure diagram of NETA chelated with radionuclide.Fig.6 Chemical structure diagram of NETA chelated with radionuclide.

We offers chelators screening and synthesis services, for lateral chelator conjugation services, including covalently binding antibodies, small molecules, and peptides to metal ions.

banner