Description

Product Description

DOTA-CXCR4-L is a specialized cyclic peptide ligand that selectively targets the C-X-C chemokine receptor type 4 (CXCR4), a G-protein-coupled receptor (GPCR) overexpressed in various tumors, including glioblastoma and triple-negative breast cancer (TNBC). This compound incorporates a DOTA chelating group, enabling stable radiolabeling with diagnostic and therapeutic isotopes such as ⁶⁸Ga, ⁶⁴Cu, or ¹⁷⁷Lu, making it an ideal platform for the synthesis of radionuclide-drug conjugates (RDCs).

CXCR4 plays a pivotal role in tumor progression, metastasis, and angiogenesis, largely through its interaction with the ligand CXCL12 (SDF-1α). By binding competitively to CXCR4, DOTA-CXCR4-L allows researchers to trace, block, or modulate CXCR4-mediated signaling pathways.

This peptide is a versatile molecular tool for nuclear imaging (PET/SPECT) and targeted radionuclide therapy (TRT) applications, enabling noninvasive visualization of CXCR4-positive tumors and therapeutic evaluation of CXCR4 antagonists.

Structural and Functional Overview

DOTA-CXCR4-L contains a macrocyclic DOTA moiety linked to a high-affinity CXCR4-binding sequence. The DOTA chelator confers strong thermodynamic stability for metal complexes, ensuring robust radiolabeling performance with minimal decomposition. Once complexed with isotopes such as ⁶⁸Ga or ¹⁷⁷Lu, the conjugate demonstrates exceptional in vivo retention and target specificity.

Because CXCR4 overexpression correlates with aggressive cancer phenotypes, DOTA-CXCR4-L enables quantitative imaging of tumor receptor density and assessment of metastatic potential. Additionally, its radiolabeled analogs can be utilized to deliver cytotoxic doses selectively to CXCR4-positive tumor tissues.

Research Significance

• Tumor Imaging: Used for noninvasive mapping of CXCR4 expression in glioblastoma, TNBC, and other metastatic cancers.

• Radionuclide Therapy Development: Facilitates creation of ¹⁷⁷Lu-labeled constructs for internal radiotherapy.

• CXCR4 Signaling Studies: Supports research on receptor trafficking, desensitization, and antagonist screening.

• Theranostics: Combines diagnostic and therapeutic capabilities for dual-function imaging and treatment research.

The broad applicability and molecular precision of DOTA-CXCR4-L make it a cornerstone in translational oncology and molecular nuclear medicine research.

Product Specifications

Mechanism of Action

DOTA-CXCR4-L acts by binding with high affinity to the CXCR4 receptor, inhibiting its interaction with the endogenous chemokine CXCL12. This receptor–ligand axis is crucial in tumor cell migration, metastasis, and chemoresistance.

Upon radiolabeling with isotopes such as ⁶⁸Ga or ¹⁷⁷Lu, the resulting complex targets CXCR4-expressing tumor cells, enabling precise localization via PET or SPECT imaging. The radioisotopic emission profile facilitates real-time monitoring of CXCR4 distribution and quantification of receptor expression.

The DOTA chelator ensures stable coordination of radiometal ions, preventing in vivo detachment and off-target accumulation. Thus, DOTA-CXCR4-L not only provides molecular-level insight into CXCR4-mediated oncogenic signaling but also serves as a modular scaffold for designing novel CXCR4-targeted theranostic agents.

Side Effects

As a research-grade compound, DOTA-CXCR4-L exhibits no known toxicity under laboratory conditions. However, radiolabeled derivatives must be handled with caution due to ionizing radiation exposure.

Observed in vitro and in vivo characteristics include:

• Minimal off-target receptor binding

• Low cytotoxicity in non-radiolabeled form

• Fast renal clearance and limited hepatobiliary retention

Proper radiation shielding, controlled handling, and adherence to institutional safety standards are recommended for experiments involving ⁶⁸Ga or ¹⁷⁷Lu labeling.

Keywords

DOTA-CXCR4-L, CXCR4 peptide ligand, CXCR4 tracer, ⁶⁸Ga-DOTA-CXCR4-L, ¹⁷⁷Lu-DOTA-CXCR4-L, radionuclide-drug conjugate, PET imaging agent, theranostic peptide, CXCR4-targeted radioligand, glioblastoma imaging compound

Shipping Guarantee

All shipments are handled using validated cold-chain logistics to preserve peptide integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

Payment Support

We provide flexible and secure global payment options to support international research transactions. Accepted payment methods include PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are protected by industry-standard encryption and verified payment gateways to ensure confidentiality and fund security.