DOTA-TATE(DOTA-[Tyr3]-Octreotate)

DOTATATE (Oxodotreotide) is an octreotate-based peptide featuring a tyrosine substitution at position 3 and a DOTA chelator for radiolabeling. The peptide-chelator complex forms a somatostatin analog ligand with very high affinity to SSTR2, a somatostatin receptor frequently overexpressed in neuroendocrine tumors (NETs). Labeled with radionuclides (e.g., Ga-68, Cu-64, Lu-177), DOTA TATE serves as a radioligand for PET/CT imaging of NETs and peptide receptor radionuclide therapy (PRRT). With its dual diagnostic-therapeutic ability and SSTR2 selectivity, DOTATATE is a gold standard agent in oncology.

Produced by JPT Peptide Technologies, a leader in custom peptide synthesis and oncology research reagents.

DOTA-TATE(DOTA-[Tyr3]-Octreotate), precursor for radiolabeled DOTA-TATE and ligand for somatostatin receptors. Can be bound to radionuclides for development of cancer treatment and diagnosis. For research use only!

DOTA-TATE(DOTA-[Tyr3]-Octreotate) - Specifications

• Peptide sequence: DPhe-Cys-Tyr-DTrp-Lys-Thr-Cys-Thr (cyclic disulfide)
• Amount: 1mg (10 x100µg)
• Purity: >95% (HPLC-MS)
• Delivery Format: Freeze-dried in glass vial
• CAS: 177943-89-4
• Application(s): Nuclear medicine
• Condition(s)/Topic(s): Cancer
• Standard Delivery Time: approx. 3 weeks

JPT Peptide Technologies provide DOTATATE in a range of aliquot sizes, ensuring flexibility for diverse research applications. For any special requirements, please contact our customer support: peptide@jpt.com

Radiolabeled DOTATATE variants and their applications:

As the backbone for its radiolabeled derivatives, DOTA TATE can be conjugated with various radionuclides through its DOTA chelator, producing highly selective radioligands for both imaging and therapy of neuroendocrine tumors (NETs). For example:

• Ga-68-DOTA-TATE is extensively employed in PET/CT imaging, providing exceptional sensitivity and accuracy in detecting SSTR2-positive tumors via positron emission tomography.
• Lu-177-DOTA-TATE and Y-90-DOTA-TATE are central to peptide receptor radionuclide therapy (PRRT), delivering targeted beta radiation directly into receptor-expressing cells and inducing tumor cell death.
• Ac-225-DOTA-TATE
is currently being evaluated for advanced or treatment-resistant cases, where its alpha emissions offer intense, localized DNA damage and therapeutic potential.

Collectively, these applications demonstrate the pivotal role of DOTA TATE radioligands in precision diagnosis and targeted therapy, cementing their status in nuclear oncology.

We also offer customized DOTA TATE tailored to your research needs (non-radioactive variants). More information is available on our website!

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Research areas and applications of DOTA-[Tyr3]-octreotate, CAS: 177943-89-4:

• Receptor expression studies: Investigated for assessing SSTR2 and SSTR5 levels in tumors, with the aim of supporting research into patient stratification and personalized therapy approaches.
• NET diagnosis and staging research: Explored for its potential to provide highly sensitive PET/CT imaging in detecting both primary neuroendocrine tumors and metastatic lesions.
• Exploration of extended tumor imaging: Studied for possible application in other SSTR2-positive cancers beyond NETs, such as pituitary, lung, and pancreatic tumors.
• PRRT treatment studies: Researched as a method to identify patients who may benefit from PRRT and to examine receptor uptake as a predictor of treatment response.
• Therapy monitoring development: Evaluated in studies aiming to follow disease progression, treatment effects, and recurrence in the context of radionuclide therapies.
• Theranostic research: Investigated as part of combined strategies that integrate diagnostic PET/CT imaging with therapeutic radionuclide delivery.
• Novel radioconjugate development: Explored as a basis for creating new radionuclide-drug conjugates designed to unify imaging and therapeutic functions.
• Biodistribution and pharmacokinetics research: Studied to better understand tracer kinetics, including tumor uptake, organ distribution, and clearance in preclinical and early clinical investigations.

Benefits of DOTA-TATE (Oxodotreotide) and its radiolabeled variants:

• High sensitivity and specificity: Accurately detects even small or early neuroendocrine tumor (NET) lesions by targeting SSTR2 with exceptional binding affinity.
• Functional imaging: Provides molecular insight by visualizing SSTR2 activity, complementing structural data from PET/CT for improved diagnostic accuracy.
• Highly selective receptor targeting: Exhibits very high selectivity and affinity for SSTR2, ensuring precise identification of receptor-positive tumors with reduced off-target binding.
• Theranostics: Embodies the theranostic concept by uniting PET/CT imaging with PRRT, enabling seamless integration of diagnosis and treatment in targeted oncology.

Key Concepts

What are radionuclides and radioligands?

Radionuclides are unstable isotopes that emit radiation as they decay, a feature that makes them highly useful in oncology. Their medical application depends on the radiation type: positron and gamma emitters provide high-resolution imaging, while beta and alpha emitters deliver localized radiation capable of destroying tumor cells.

When a radionuclide is coupled to a molecule (ligand) that binds specifically to certain receptors or cells, the compound formed is called a radioligand. Radioligands combine the selective targeting ability of the ligand with the diagnostic or therapeutic properties of the radionuclide, enabling precise tumor imaging and targeted therapy.

What is Peptide Receptor Radionuclide Therapy?

Peptide Receptor Radionuclide Therapy (PRRT) is a targeted therapeutic approach most often applied to neuroendocrine tumors (NETs) that strongly express somatostatin receptors. In this method, somatostatin analogs such as octreotide derivatives are chemically attached to a radionuclide (typically lutetium-177 or yttrium-90) using the DOTA chelator.

After injection, the radiolabeled peptide binds with high affinity to somatostatin receptors on tumor cells and is taken up through receptor-mediated internalization. This process enables the radionuclide to release ionizing radiation directly inside malignant tissue while limiting damage to neighboring healthy cells. By exploiting this receptor-specific delivery, PRRT supports tumor reduction and disease control, and is recognized as an effective treatment option for patients with advanced or metastatic NETs.

What is a DOTA chelator?

A DOTA chelator (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) is a macrocyclic molecule designed to tightly bind metal ions, including radionuclides such as Ga-68, Lu-177, and Y-90. Acting like a molecular cage, DOTA securely holds the radionuclide within the peptide structure in vivo, preventing its premature release and reducing off-target radiation. This strong binding is essential for both precise tumor targeting and patient safety, as it ensures the radioligand remains stable in circulation until it reaches receptor-positive tumor tissue.

Impact of Tyr3 Substitution on Receptor Affinity

DOTA-TATE peptide is derived from octreotate, a close analog of octreotide that carries a threonine at the C-terminus, which improves binding stability compared to the original octreotide scaffold. Within this backbone, the tyrosine (Tyr3) substitution introduces a polar aromatic residue that further strengthens receptor interaction. These combined modifications confer very high affinity and selectivity for SSTR2. Thus, DOTA TATE provides highly precise targeting of SSTR2-positive tumors and is a gold standard agent in both imaging and peptide receptor radionuclide therapy (PRRT) of neuroendocrine tumors.

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