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AS1411-G2(DTPA-Gd)-SS-PR
- Development stage
- Preclinical
- Modality
- RNA Aptamers → RNA Therapeutics → Nucleic Acid Therapeutics, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Nanoparticles → Drug Delivery Systems, DNA Aptamers → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous
01
Overview
AS1411-G2(DTPA-Gd)-SS-PR is an aptamer-conjugated polyrotaxane-based macromolecular MRI contrast agent designed for targeted imaging of nucleolin-overexpressing tissues, particularly cancer cells[1][2]. It comprises the anti-nucleolin aptamer AS1411 conjugated to a polyrotaxane (PR) backbone via a disulfide (SS) linker, with multiple G2(DTPA-Gd) (gadolinium-diethylenetriaminepentaacetate) chelators attached for enhanced magnetic resonance imaging performance[1][5]. This agent leverages the specific binding of AS1411 to nucleolin, a protein overexpressed on the surface of many tumor cells, enabling selective accumulation and prolonged contrast imaging at the tumor site[1][2]. It has demonstrated superior biocompatibility and reduced accumulation-associated toxicity in preclinical models[2]. The longitudinal relaxivity is approximately 11.7 mM⁻¹s⁻¹, which is about twice that of clinically used Gd-DTPA[6].
- Other names
- AS1411-G2(DTPA-Gd)-SS-PRAS1411-G2(chelate-Gd)-SS-PR
02
Targets
NCL (Nucleolin)
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