FAPI-2
Based on 1 Customer Validation
FAPI-2 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 has advantages such as fast tracer kinetics, no need for fasting preparation, and being unaffected by blood glucose.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.94%
- No. CAS: 2370952-98-8
- Fòrmula: C40H56N10O10
- Peso molecular:836.93
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Fibroblast activation protein (FAP)[1]
FAPI-2 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
-
No. CAS 2370952-98-8
-
Appearance Solid
-
Peso molecular 836.93
-
Fòrmula C40H56N10O10
-
Color White to off-white
-
SMILES
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (119.48 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)
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: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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.
Pureza y Documentación
-
Ficha de datos (272 KB)
-
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)
-
Instrucciones de manejo (2659 KB)
Referencias
[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. 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 | 1.1948 mL | 5.9742 mL | 11.9484 mL | 29.8711 mL |
| 5 mM | 0.2390 mL | 1.1948 mL | 2.3897 mL | 5.9742 mL | |
| 10 mM | 0.1195 mL | 0.5974 mL | 1.1948 mL | 2.9871 mL | |
| 15 mM | 0.0797 mL | 0.3983 mL | 0.7966 mL | 1.9914 mL | |
| 20 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4936 mL | |
| 25 mM | 0.0478 mL | 0.2390 mL | 0.4779 mL | 1.1948 mL | |
| 30 mM | 0.0398 mL | 0.1991 mL | 0.3983 mL | 0.9957 mL | |
| 40 mM | 0.0299 mL | 0.1494 mL | 0.2987 mL | 0.7468 mL | |
| 50 mM | 0.0239 mL | 0.1195 mL | 0.2390 mL | 0.5974 mL | |
| 60 mM | 0.0199 mL | 0.0996 mL | 0.1991 mL | 0.4979 mL | |
| 80 mM | 0.0149 mL | 0.0747 mL | 0.1494 mL | 0.3734 mL | |
| 100 mM | 0.0119 mL | 0.0597 mL | 0.1195 mL | 0.2987 mL |
FAPI-2 Related Classifications
HY-128642 Related Classifications
Powered by Bioz