NH2-UAMC1110 

NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose-response, and has been used for tumor diagnosis. NH2-UAMC1110 introduces an active amino group into its structure, enabling it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.), thereby synthesizing molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling processes. Its key activity is high targeting and high affinity, and its core function is to be coupled with bifunctional chelators (such as DOTA, DATA5m) as a targeting module. NH2-UAMC1110 can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis^[1][2].

NH2-UAMC1110 was coupled with DOTA.SA in phosphate buffer at pH 9 to successfully synthesize the FAP-targeting probe DOTA.SA.FAPi. The product was purified by HPLC to achieve the required purity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

431.44

C₂₁H₂₃F₂N₅O₃

2758337-19-6

Solid

White to off-white

O=C(N1[C@@H](CC(F)(C1)F)C#N)CNC(C2=CC=NC3=C2C=C(OCCCCN)C=C3)=O

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Moon ES, et al. Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATA5m chelators. EJNMMI Radiopharm Chem. 2020 Jul 29;5(1):19.  [Content Brief]

  [2]. Mirzaei A, et al. FAP Inhibitors as Novel Small Molecules for Cancer Imaging using Radionuclide[J]. Journal of Radiopharmaceuticals and Molecular Probes, 2023, 9(1): 49-55.