FAPI-74
Based on 1 Customer Validation
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.
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- Pureté: 99.82%
- CAS No.: 2374782-76-8
- Formule: C36H49N9O8
- Masse moléculaire:735.83
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
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.
Chemical Information
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CAS No. 2374782-76-8
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Appearance Solid
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Masse moléculaire 735.83
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Formule C36H49N9O8
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Color Off-white to light yellow
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SMILES
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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (169.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3590 mL | 6.7950 mL | 13.5901 mL | 33.9752 mL |
| 5 mM | 0.2718 mL | 1.3590 mL | 2.7180 mL | 6.7950 mL | |
| 10 mM | 0.1359 mL | 0.6795 mL | 1.3590 mL | 3.3975 mL | |
| 15 mM | 0.0906 mL | 0.4530 mL | 0.9060 mL | 2.2650 mL | |
| 20 mM | 0.0680 mL | 0.3398 mL | 0.6795 mL | 1.6988 mL | |
| 25 mM | 0.0544 mL | 0.2718 mL | 0.5436 mL | 1.3590 mL | |
| 30 mM | 0.0453 mL | 0.2265 mL | 0.4530 mL | 1.1325 mL | |
| 40 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8494 mL | |
| 50 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6795 mL | |
| 60 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL | |
| 80 mM | 0.0170 mL | 0.0849 mL | 0.1699 mL | 0.4247 mL | |
| 100 mM | 0.0136 mL | 0.0680 mL | 0.1359 mL | 0.3398 mL |