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.
For research use only. We do not sell to patients.
- Purity : 99.82%
- CAS No.: 2374782-76-8
- Formula: C36H49N9O8
- Molecular Weight:735.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
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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Molecular Weight 735.83
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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
| 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 |