FAPI-74 

FAPI-74 is a PET (positron emission tomography) tracer targeting the fibroblast activation protein (FAP). FAPI-74 can be used for FAP-positive tumor research^[1][2].

Chelation with ¹⁸F-AlF^[2]
2-10 GBq ¹⁸F fluoride in 4 mL water were trapped on an anion exchange cartridge and eluted with 0.30 mL 0.5 M NaOAc pH 3.9. The solution was incubated with 6 µL of AlCl3 in water (10 mM) and 300 µL dimethyl sulfoxide for 5 min at room temperature before 20 µL of a solution of FAPI-74 (4 mM) were added. The reaction was carried out at 95 °C for 15 min, cooled to room temperature, diluted with 5 mL water and worked up by SPE. The final product was eluted with 0.5 mL ethanol, 5 mL 0.9% saline and spiked with phosphate buffer before sterile filtration. Chelation with 68Ga was achieved by adding 1.00 mL 68Ge/68Ga-generator eluate (0.6 M hydrochloric adic; ca. 1.2 GBq) to a mixture of 15 µL FAPI-74 solution (4 mM in water), 310 µL sodium acetate (2.5 M in water) and 0.50 mL ethanol.
PET/CT Imaging to assist tumor volume delineation for guiding radiotherapy with lung cancer^[3]
PET images were acquired with a small animal PET scanner 3 weeks after the implantation in PANC-1 xenograft mice (9 weeks old, body weight=25.3±1.2 g, n=9). Under 2% isofurane anesthesia, [¹⁸F]FAPI-74 (12.4±1.7 MBq) was injected in the tail vein. Dynamic PET scans (scan duration=70 min, n=2) were started simultaneously with the bolus injection. Static PET scans (scan duration=10 min, n=7) were performed 1 h after injection, followed by a CT scan.

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

735.83

C₃₆H₄₉N₉O₈

2374782-76-8

Solid

Off-white to light yellow

O=C(C1=CC=NC(C=C2)=C1C=C2OCCCN(CC3)CCN3C(CN(CCN4CC(O)=O)CCN(CC4)CC(O)=O)=O)NCC(N(CCC5)[C@@H]5C#N)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Uwe Haberkorn, et al. Fap inhibitor. Patent, WO2019154886A1.

  [2]. Giesel FL, et al. FAPI-74 PET/CT Using Either 18F-AlF or Cold-Kit 68Ga Labeling: Biodistribution, Radiation Dosimetry, and Tumor Delineation in Lung Cancer Patients. J Nucl Med. 2021 Feb;62(2):201-207.  [Content Brief]

  [3]. Liu Y, et al. Fibroblast activation protein targeted therapy using [177Lu]FAPI-46 compared with [225Ac]FAPI-46 in a pancreatic cancer model. Eur J Nucl Med Mol Imaging. 2022 Feb;49(3):871-880.  [Content Brief]