FAPI-mFS
Based on 1 Customer Validation
FAPI-mFS is a selective fibroblast activation protein (FAP) inhibitor with an IC50 of 0.0014 μM against human FAP. Through its covalent binding property with FAP, FAPI-mFS enhances its uptake and retention time in cancer cells. When radiolabeled with 68Ga, FAPI-mFS serves as a PET/CT imaging agent with superior tumor-to-background tissue contrast and lesion detection capability. When radiolabeled with 177Lu or 225Ac, FAPI-mFS induces tumor regression and inhibition in preclinical models. FAPI-mFS can be used in studies related to cancer and radionuclide-conjugated drugs (RDC).
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- Purity: 98.71%
- CAS No.: 3023869-94-2
- 화학식: C53H69F3N12O15S
- 분자량:1203.25
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보관:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* 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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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Radionuclide-Drug Conjugates (RDCs) Isoforms
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Biological Activity
FAPI-mFS binds to purified human FAP with high affinity (KD = 1.47×10-12 M). Its association rate is 15 times faster than that of FAPI-04, and its dissociation rate is extremely slow, suggesting irreversible binding[1].
FAPI-mFS exhibits rapid and efficient uptake in HT-1080-FAP cells, and forms stable covalent bonds with intracellular FAP[1].
FAPI-mFS potently inhibits the activity of purified FAP enzyme (IC50 = 1.4×10-3 μM) and exhibits high selectivity toward homologous prolyl oligopeptidases DPP-4 and PREP[1].
FAPI-mFS binds persistently to excised human MTC tumor tissues, with no significant dissociation after incubation in blank solution for 24 h[1].
FAPI-mFS competes with [68Ga]Ga-FAPI-04 for binding to HT-1080-FAP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3023869-94-2
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Appearance Solid
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분자량 1203.25
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화학식 C53H69F3N12O15S
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Color White to off-white
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : ≥ 100 mg/mL (83.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.5 mg/mL (2.08 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 (2.08 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:
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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.
순도&문서
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Cui XY, et al. Covalent targeted radioligands potentiate radionuclide therapy. Nature. 2024 Jun;630(8015):206-213. [Content Brief]
[2]. Luo Y, et al. Based on small molecules: development and application of fibroblast activation protein inhibitors radiopharmaceutical in tumor precision therapy. Frontiers in pharmacology. 2025;16:1593380. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.8311 mL | 4.1554 mL | 8.3108 mL | 20.7771 mL |
| 5 mM | 0.1662 mL | 0.8311 mL | 1.6622 mL | 4.1554 mL | |
| 10 mM | 0.0831 mL | 0.4155 mL | 0.8311 mL | 2.0777 mL | |
| 15 mM | 0.0554 mL | 0.2770 mL | 0.5541 mL | 1.3851 mL | |
| 20 mM | 0.0416 mL | 0.2078 mL | 0.4155 mL | 1.0389 mL | |
| 25 mM | 0.0332 mL | 0.1662 mL | 0.3324 mL | 0.8311 mL | |
| 30 mM | 0.0277 mL | 0.1385 mL | 0.2770 mL | 0.6926 mL | |
| 40 mM | 0.0208 mL | 0.1039 mL | 0.2078 mL | 0.5194 mL | |
| 50 mM | 0.0166 mL | 0.0831 mL | 0.1662 mL | 0.4155 mL | |
| 60 mM | 0.0139 mL | 0.0693 mL | 0.1385 mL | 0.3463 mL | |
| 80 mM | 0.0104 mL | 0.0519 mL | 0.1039 mL | 0.2597 mL |
FAPI-mFS Related Classifications
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