1,4,7-triazacyclononane-N,N',N''-triacetic acid
It is used as a chelating agent and in the preparation of radiopharmaceuticals for medical imaging and therapy.
This versatile molecule has applications in chemistry, biology, and medicine.
Most cited protocols related to «1,4,7-triazacyclononane-N,N',N''-triacetic acid»
Most recents protocols related to «1,4,7-triazacyclononane-N,N',N''-triacetic acid»
Example 9
In vivo PET/CT imaging was conducted in NCr nude mice bearing bxpc3 (human pancreatic adenocarcinoma cell line) and 4T1 (a murine breast cancer cell line that overexpresses integrin αvβ3 and CD13) tumor xenografts.
Mice were injected with bxpc3 cells (1 million cells in 150 μL PBS) into the subcutaneous flank of the right shoulder and 4T1 cells (1 million cells in 150 μL PBS) into the subcutaneous flank of the left shoulder. Either the CNGRC-(68Ga)NOTA-RGDyK heterodimer (“CNGRC” disclosed as SEQ ID NO: 1), (68Ga)NOTA(CNGRC) (“CNGRC” disclosed as SEQ ID NO: 1), or (68Ga)NOTA(RGDyK) were injected into the bloodstream via tail vein injection. Blocking studies were conducted for the heterodimer studies by co-injecting 100 times of cyclo(CNGRC) (“CNGRC” disclosed as SEQ ID NO: 1) and cyclo(RGDyK). Small animal PET/CT was performed at 1 hour post injection of tracers (
Example 14
Eight NH2—PEGn-RGD peptides containing spacers of various PEG lengths (n=2, 4, 6, 8, 10, 12, 14, 16) will be prepared by adding the corresponding Boc-PEGn-NHS to RGD in a PBS buffer (pH=8.2), followed by Boc deprotection. Photo-ODIBO-NHS, prepared using previously reported procedures, will then be mixed with the prepared NH2—PEGn-RGD in a PBS buffer (pH=8.2) to produce photo-OIDBO-PEGn-RGD. N3-PEG4-cetuximab will be prepared using previously reported procedures. N3—PEG4-cetuximab and the eight photo-ODIBO-PEGn-RGD peptides (n=2, 4, 6, 8, 10, 12, 14, 16) will be used for in vitro screening (at 4° C. to minimize the internalization of targeting probes). As shown in
The ODIBO-PEGn-RGD containing the most potent PEG spacer will click with Tz-NOTA-N3 and then be radiolabeled with 64Cu, and the resulting Tz-(64Cu)NOTA-PEGn-RGD will be used for the in vitro avidity studies on U87MG cells. Tz-(64Cu)NOTA-RGD (without a PEG spacer) will be used as a negative control because the distance between RGD and cetuximab in the resulting heterodimer is too short to achieve avidity effect (proved in preliminary study,
Various references are cited in this document, which are hereby incorporated by reference in their entireties herein.
Example 10
In vivo PET/CT imaging was conducted in Balb/c mice. One week after the orthotropic implantation of 1×106 luciferase-transfected KPCP cancer cells into the pancreas of Balb/c mice, the mice were used for PET imaging. Either the CNGRC-(68Ga)NOTA-RGDyK heterodimer (“CNGRC” disclosed as SEQ ID NO: 1), (68Ga)NOTA(CNGRC) (“CNGRC” disclosed as SEQ ID NO: 1), or (68Ga)NOTA(RGDyK)] were injected into the bloodstream via tail vein injection. Blocking studies were conducted for the heterodimer studies by co-injecting 100× of CNGRC (SEQ ID NO: 1) and RGDyK. Small animal PET/CT was performed at 1 hour post injection of tracers (
Standardized Uptake Value (SUV, normalized radiotracer uptake by body weight and injected tracer dose)35 (link) was calculated for regions of interest (ROIs) defined over focal uptakes of the ZD2 ligand as well as a nearby ROI over the liver background away from focal uptakes, similar to that used for computing FDG uptake.36 (link) Time activity curves in the unit of SUV were generated for these ROIs.
Top products related to «1,4,7-triazacyclononane-N,N',N''-triacetic acid»
More about "1,4,7-triazacyclononane-N,N',N''-triacetic acid"
This versatile molecule, also known as p-SCN-Bn-NOTA, has a wide range of applications in chemistry, biology, and medicine.
As a chelating agent, NOTA is commonly used in the preparation of radiopharmaceuticals for medical imaging and therapy.
The compound's ability to form stable complexes with various metal ions, such as gallium-68 (68Ga) from a 68Ge/68Ga generator, makes it useful for labeling biomolecules like peptides and antibodies for positron emission tomography (PET) imaging.
In the laboratory, NOTA can be purified using a Chelex 100 resin column, and its concentration can be determined using a gamma counter.
The compound can also be conjugated to larger molecules, such as polyethylene glycol (PEG), to create constructs like S-2-(4-isothiocyanatobenzyl)-1,4,7-triazacyclononane-1,4,7-triacetic acid (p-SCN-Bn-NOTA), which can be used for further functionalization or labeling.
NOTA's versatility extends to its use in small animal imaging, where it has been employed in Inveon rodent model scanners to study various biological processes and disease models.
The compound can also be desalted using a PD-10 desalting column before further analysis or application.
Overall, 1,4,7-Triazacyclononane-N,N',N''-Triacetic Acid (NOTA) is a powerful tool in the fields of chemistry, biology, and medicine, with a wide range of uses and the potential for further development and innovation.