FAPI-2 TFA
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 98.05%
- Formula: C42H57F3N10O12
- Molecular Weight:950.96
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
FAPI-2 TFA has advantages such as fast tracer kinetics (imaging can be performed in less than 1 hour after injection), low background in the liver, oral mucosa, and brain, and being unaffected by blood glucose. Moreover, the DOTA chelator it contains can be labeled with multiple therapeutic radionuclides[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 950.96
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Formula C42H57F3N10O12
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Color Off-white to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 200 mg/mL (210.31 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (5.26 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (5.26 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (271 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]. 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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 1.0516 mL | 5.2578 mL | 10.5157 mL | 26.2892 mL |
| 5 mM | 0.2103 mL | 1.0516 mL | 2.1031 mL | 5.2578 mL | |
| 10 mM | 0.1052 mL | 0.5258 mL | 1.0516 mL | 2.6289 mL | |
| 15 mM | 0.0701 mL | 0.3505 mL | 0.7010 mL | 1.7526 mL | |
| 20 mM | 0.0526 mL | 0.2629 mL | 0.5258 mL | 1.3145 mL | |
| 25 mM | 0.0421 mL | 0.2103 mL | 0.4206 mL | 1.0516 mL | |
| 30 mM | 0.0351 mL | 0.1753 mL | 0.3505 mL | 0.8763 mL | |
| 40 mM | 0.0263 mL | 0.1314 mL | 0.2629 mL | 0.6572 mL | |
| 50 mM | 0.0210 mL | 0.1052 mL | 0.2103 mL | 0.5258 mL | |
| 60 mM | 0.0175 mL | 0.0876 mL | 0.1753 mL | 0.4382 mL | |
| 80 mM | 0.0131 mL | 0.0657 mL | 0.1314 mL | 0.3286 mL | |
| 100 mM | 0.0105 mL | 0.0526 mL | 0.1052 mL | 0.2629 mL |
FAPI-2 TFA Related Classifications
HY-128642A Related Classifications
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