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.

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

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.

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.

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. 

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.

Fig.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.

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.

Our Service

• Chelator Screening Service
  With more than 10 kinds of chelators, we can provide customized chelator synthesis, analysis, and screening services for your specific complex with fewer effects on biological activity.
• Chelator Synthesis Service
  The chelator is one of the most important parts of RDC. Rdcthera has a professional team, grouped by excellent chemists. Our custom chelator synthesis service can supply quantities ranging from milligrams to hundred grams. In addition to developing an optimized synthesis route, we can also synthesize chelators through your own process.
• Synthesis Path Optimization Service
  We can optimize and modify the chelating agents with the most efficient synthesis path and guarantee high-quality and extreme purity chelators for lateral conjugations.

Project Workflow

Why Choose Us

Rdcthera has been working on chelator development for years. We are professionals at chelator design, screening, and synthesis. After chelator synthesis, we can offer you RDC conjugation service and RDC analysis service as well.

Industrial Leadership

Cost Efficient

Highly Customizable

Premium Quality

We are honored to share our experience, acknowledgment, and technology with you and help you screen for the best-fit chelator for your RDC. Please contact us for more information.

• Radionuclide Generation and Screening Service
• Radiolabelling Services
• Linker Design and Synthesis Service
• RDC Cargo Development Service