FAPI-4
Based on 32 publication(s) in Google Scholar
FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.
For research use only. We do not sell to patients.
- Purity: 99.47%
- CAS No.: 2374782-02-0
- Formula: C40H54F2N10O10
- Molecular Weight:872.91
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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
Publications Citing Use of MedChemExpress (MCE) FAPI-4
More- Radiology. 2023 Jun;307(5):e222448. [Abstract]
- Radiology. 2022 Sep;304(3):648-657. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(19):e21279. [Abstract]
- Eur J Nucl Med Mol Imaging. 2022 Feb;49(3):963-979. [Abstract]
- Eur J Nucl Med Mol Imaging. 2021 Oct;48(11):3493-3501. [Abstract]
- Biomed Pharmacother. 2025 Apr 16:187:118048. [Abstract]
- Molecules. 2024 Nov 19;29(22):5457. [Abstract]
- Mol Pharm. 2025 Oct 6;22(10):6247-6257. [Abstract]
- Mol Pharm. 2025 Feb 3;22(2):906-917. [Abstract]
- Mol Pharm. 2023 Dec 4;20(12):6441-6450. [Abstract]
- Mol Pharm. 2023 May 1;20(5):2714-2725. [Abstract]
- Sci Rep. 2026 Jan 7;16(1):4410. [Abstract]
- Sci Rep. 2026 Jan 11;16(1):5031. [Abstract]
- Br J Radiol. 2024 Mar 28;97(1156):859-867. [Abstract]
- Diagnostics (Basel). 2025 Dec 19;16(1):10. [Abstract]
- Front Oncol. 2022 Jun 16;12:875081. [Abstract]
- EJNMMI Radiopharm Chem. 2021 Apr 16;6(1):16. [Abstract]
- Mol Imaging Biol. 2022 Oct;24(5):789-797. [Abstract]
- Ann Nucl Med. 2021 Dec;35(12):1321-1331. [Abstract]
- Tomography. 2022 Feb 1;8(1):293-302. [Abstract]
- Braz J Otorhinolaryngol. 2025 Sep 6;91(6):101703. [Abstract]
- J Radioanal Nucl Chem. 2024 May 13.
- Nucl Med Commun. 2023 Mar 1;44(3):194-203. [Abstract]
- Nuklearmedizin. 2023 Feb;62(1):38-44. [Abstract]
- World J Nucl Med. 2025.
- Research Square Preprint. 2023 Jun 15.
- Springer. 2023 Apr 12.
- Research Square Preprint. 2022 May.
- Research Square Preprint. 2021 Aug.
- Research Square Preprint. 2021 Aug.
- Research Square Preprint. 2021 Jun.
- Research Square Preprint. 2021 Mar.
Biological Activity
Fibroblast activation protein (FAP)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8-week-old BALB/c nu/nu mice inoculated with HT-1080-FAP cells[2]
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Dosage:30 nmol per mouse
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Administration:Intravenous injection; 30 nmol per mouse; once
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Result:Revealed the high overall tumor uptake (9.44%ID/g 4 h after injection).
Chemical Information
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CAS No. 2374782-02-0
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Appearance Solid
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Molecular Weight 872.91
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Formula C40H54F2N10O10
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Color White to off-white
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SMILES
O=C(NCC(N1CC(F)(F)C[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
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (32)
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Journal Impact Factor
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Most Recent
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Radiology
2023 Jun;307(5):e222448. PMID: 37219440 -
Radiology
Prospective Comparison of 68Ga-FAPI versus 18F-FDG PET/CT for Tumor Staging in Biliary Tract Cancers. [Abstract]2022 Sep;304(3):648-657. PMID: 35579524 -
Adv Sci (Weinh)
Mapping CSC-Mediated Ovarian Cancer Chemoresistance via CXCR4-PET to Guide Precision Cisplatin Re-Sensitization Therapy. [Abstract]2026 Apr;13(19):e21279. PMID: 41632105 -
Eur J Nucl Med Mol Imaging
The potential utility of [68 Ga]Ga-DOTA-FAPI-04 as a novel broad-spectrum oncological and non-oncological imaging agent-comparison with [18F]FDG. [Abstract]2022 Feb;49(3):963-979. PMID: 34410435 -
Eur J Nucl Med Mol Imaging
2021 Oct;48(11):3493-3501. PMID: 33829416 -
Biomed Pharmacother
Feasibility assessment of radiolabeled FAPI-04 for diagnostic and therapeutic use in rheumatoid arthritis. [Abstract]2025 Apr 16:187:118048. PMID: 40245546 -
Molecules
Towards a General Method for Using Cyclotron-Produced Ga68 to Manufacture Clinical and Research Ga68 Tracers. [Abstract]2024 Nov 19;29(22):5457. PMID: 39598846 -
Mol Pharm
Synthesis, Radiolabeling, and Evaluation of a Dimeric Fibroblast Activation Protein Inhibitor with a Triazine Linker. [Abstract]2025 Oct 6;22(10):6247-6257. PMID: 40893020 -
Mol Pharm
Comparative Study of Dimeric Fibroblast Activation Protein-Targeting Radioligands Labeled with Fluorine-18, Copper-64, and Gallium-68. [Abstract]2025 Feb 3;22(2):906-917. PMID: 39736080 -
Mol Pharm
Synthesis and Evaluation of [18F]SiFA-Conjugated Ligands for Fibroblast Activation Protein Imaging. [Abstract]2023 Dec 4;20(12):6441-6450. PMID: 37968928 -
Mol Pharm
Noninvasive Assessment of Renal Fibrosis of Chronic Kidney Disease in Rats by [68Ga]Ga-FAPI-04 Small Animal PET/CT and Biomarkers. [Abstract]2023 May 1;20(5):2714-2725. PMID: 37010328 -
Sci Rep
Superior mucoepidermoid carcinoma detection with ⁶⁸Ga-FAPI PET/CT reflects FAP-α expression and MAML2 fusion status. [Abstract]2026 Jan 7;16(1):4410. PMID: 41501171 -
Sci Rep
A pilot human-based study of 68Ga-FAPI-04 PET/CT in staging liver fibrosis and preliminary comparison to FIB-4 and fibroscan. [Abstract]2026 Jan 11;16(1):5031. PMID: 41521232 -
Br J Radiol
2024 Mar 28;97(1156):859-867. PMID: 38290775 -
Diagnostics (Basel)
Assessment of the Diagnostic Value of [68Ga]Ga-FAPI-04 and [18F]FDG PET in a PHMG-p-Induced Pulmonary Fibrosis Murine Model. [Abstract]2025 Dec 19;16(1):10. PMID: 41515504 -
Front Oncol
2022 Jun 16;12:875081. PMID: 35785188 -
EJNMMI Radiopharm Chem
Fully-automated synthesis of 177Lu labelled FAPI derivatives on the module modular lab-Eazy. [Abstract]2021 Apr 16;6(1):16. PMID: 33864154 -
Mol Imaging Biol
Comparison of 68Ga-FAPI PET/CT and 18FDG PET/CT Modalities in Gastrointestinal System Malignancies with Peritoneal Involvement. [Abstract]2022 Oct;24(5):789-797. PMID: 35411447 -
Ann Nucl Med
Superiority of 68Ga-FAPI PET/CT scan in detecting additional lesions compared to 18FDG PET/CT scan in breast cancer. [Abstract]2021 Dec;35(12):1321-1331. PMID: 34436740 -
Tomography
Comparison of [68Ga]-FAPI PET/CT and [18F]-FDG PET/CT in Multiple Myeloma: Clinical Experience. [Abstract]2022 Feb 1;8(1):293-302. PMID: 35202189 -
Braz J Otorhinolaryngol
Effects of fibroblasts-derived exosomal FAP in regulating EMT in epithelial cells from chronic rhinosinusitis. [Abstract]2025 Sep 6;91(6):101703. PMID: 40916258 -
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Nucl Med Commun
Comparison of 68Ga-FAPI-04 and fluorine-18-fluorodeoxyglucose PET/computed tomography in the detection of ovarian malignancies. [Abstract]2023 Mar 1;44(3):194-203. PMID: 36472415 -
Nuklearmedizin
2023 Feb;62(1):38-44. PMID: 36746149 -
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Solvent & Solubility
DMSO : 100 mg/mL (114.56 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 (stored under nitrogen). 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 (stored under nitrogen). 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 (2.86 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 (2.86 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: Saline
Solubility: 4 mg/mL (4.58 mM); Clear solution; Need ultrasonic
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 (stored under nitrogen)
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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 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]. Anastasia Loktev, et al. Development of Fibroblast Activation Protein-Targeted Radiotracers with Improved Tumor Retention. J Nucl Med. 2019 Oct;60(10):1421-1429. [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 (stored under nitrogen). 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 | 1.1456 mL | 5.7280 mL | 11.4559 mL | 28.6398 mL |
| 5 mM | 0.2291 mL | 1.1456 mL | 2.2912 mL | 5.7280 mL | |
| 10 mM | 0.1146 mL | 0.5728 mL | 1.1456 mL | 2.8640 mL | |
| 15 mM | 0.0764 mL | 0.3819 mL | 0.7637 mL | 1.9093 mL | |
| 20 mM | 0.0573 mL | 0.2864 mL | 0.5728 mL | 1.4320 mL | |
| 25 mM | 0.0458 mL | 0.2291 mL | 0.4582 mL | 1.1456 mL | |
| 30 mM | 0.0382 mL | 0.1909 mL | 0.3819 mL | 0.9547 mL | |
| 40 mM | 0.0286 mL | 0.1432 mL | 0.2864 mL | 0.7160 mL | |
| 50 mM | 0.0229 mL | 0.1146 mL | 0.2291 mL | 0.5728 mL | |
| 60 mM | 0.0191 mL | 0.0955 mL | 0.1909 mL | 0.4773 mL | |
| 80 mM | 0.0143 mL | 0.0716 mL | 0.1432 mL | 0.3580 mL | |
| 100 mM | 0.0115 mL | 0.0573 mL | 0.1146 mL | 0.2864 mL |
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