FAPI-2 (TFA)

FAPI-2 TFA is a quinoline-based fibroblast activation protein (FAP) -targeting ligand that can be labeled as 68Ga-FAPI-2 and used as a PET tracer for cancer diagnosis. FAPI-2 TFA has advantages such as fast tracer kinetics, no need for fasting preparation, and being unaffected by blood glucose[1][2][3][4].

Product Specifications

UNSPSC

12352005

Target

FAP

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/fapi-2-tfa.html

Purity

98.05

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

OC(C(F)(F)F)=O.O=C(NCC(N1CCC[C@]1(C#N)[H])=O)C2=CC=NC3=CC=C(OCCCN4CCN(C(CN5CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC5)=O)CC4)C=C32

Molecular Formula

C42H57F3N10O12

Molecular Weight

950.96

References & Citations

[1]Giesel FL, et al. 68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers. J Nucl Med. 2019 Mar;60 (3) :386-392.|[2]Moon ES, et al. Fibroblast Activation Protein (FAP) targeting homodimeric FAP inhibitor radiotheranostics: a step to improve tumor uptake and retention time. Am J Nucl Med Mol Imaging. 2021 Dec 15;11 (6) :476-491.|[3]Li M, et al. Clinical summary of fibroblast activation protein inhibitor-based radiopharmaceuticals: cancer and beyond. Eur J Nucl Med Mol Imaging. 2022 Jul;49 (8) :2844-2868. doi: 10.1007/s00259-022-05706-y. Epub 2022 Jan 31. Erratum in: Eur J Nucl Med Mol Imaging. 2022 Jul;49 (8) :3007.|[4]Sanjana Ballal, et al. First-in-Human Experience With 177Lu-DOTAGA. (SA.FAPi) 2 Therapy in an Uncommon Case of Aggressive Medullary Thyroid Carcinoma Clinically Mimicking as Anaplastic Thyroid Cancer. Clin Nucl Med. 2022 Jun 1;47 (6) :e444-e445.