DOTA-NI-FAPI-04

DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM) . By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact[1].

Product Specifications

CAS Number

[3078291-78-5]

UNSPSC

12352005

Target

FAP

Related Pathways

Immunology/Inflammation

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(CN1CCN(CCN(CCN(CC1)CC(O)=O)CC(O)=O)CC(N[C@@H](CCC(NCCCN2C=CN=C2[N+]([O-])=O)=O)C(N3CCN(CCCOC4=CC=C(C5=C4)N=CC=C5C(NCC(N6[C@@H](CC(F)(C6)F)C#N)=O)=O)CC3)=O)=O)O

Molecular Formula

C51H69F2N15O14

Molecular Weight

1154.18

References & Citations

[1]Luo Y, et al. Development of [68Ga]Ga/[177Lu]Lu-DOTA-NI-FAPI-04 Containing a Nitroimidazole Moiety as New FAPI Radiotracers with Improved Tumor Uptake and Retention. J Med Chem. 2025 Jan 9;68 (1) :348-360.