Rofapitide tetraxetan
Based on 7 publication(s) in Google Scholar
Rofapitide tetraxetan (FAP-2286) is a potent and selective FAP-binding peptide with a mean IC50 value of 2.7 nM for binding to FAP. Rofapitide tetraxetan can be labeled with radionuclides for diagnostic applications. Rofapitide tetraxetan has antitumor activity.
For research use only. We do not sell to patients.
- Purity: 99.54%
- CAS No.: 2581741-18-4
- Formula: C67H99N13O18S3
- Molecular Weight:1470.77
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, 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) Rofapitide tetraxetan
More- Radiother Oncol. 2025 Oct 4:213:111195. [Abstract]
- Pharmaceuticals (Basel). 2024 Aug 29;17(9):1141. [Abstract]
- Bioorg Chem. 2025 Nov:166:109185. [Abstract]
- Sci Rep. 2025 Mar 3;15(1):7475. [Abstract]
- EJNMMI Res. 2026 Jan 9;16(1):29. [Abstract]
- Nucl Med Biol. 2025 Oct 10:150-151:109571. [Abstract]
- Res Sq. 2025 Dec 22.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Histological Imaging/Staining
Biological Activity
Rofapitide tetraxetan (0.1-30 nM, 1 h) reduces fuorophore-labeled competitor peptide bound to cells in human WI-38 fibroblast like fetal lung cell line[1].
Rofapitide tetraxetan (5 nM, 1, 3, 8, 24, and 72 h) maintains long tumor retention and suppression in HEK-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.
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Animal Model:HEK-FAP tumor-bearing mice[1]
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Dosage:30 MBq/nmol
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Administration:Intravenous injection (i.v.)
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Result:Increased tumor-to-kidney (T/K) ratio with the highest differential uptake of 7.5 T/K obtained at 48 h post injection.
Maintained accumulation at 3 h after injection with 10.8 ID/g.
Chemical Information
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CAS No. 2581741-18-4
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Appearance Solid
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Molecular Weight 1470.77
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Formula C67H99N13O18S3
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Color White to off-white
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SMILES
O=C(N1[C@@](C(N[C@@](C(N[C@H](C(N[C@H](C2=O)CC3=CC=CC=C3)=O)CCC(N)=O)=O)([H])[C@H](O)C)=O)([H])CCC1)[C@@](CCC4)([H])N4C([C@H](CSCC5=CC(CSCCNC(CN(CCN(CC6)CC(O)=O)CCN(CCN6CC(O)=O)CC(O)=O)=O)=CC(CSC[C@H](N2)C(O)=O)=C5)NC(CCCCC)=O)=O
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Synonyms
FAP-2286
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (7)
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Journal Impact Factor
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Most Recent
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Radiother Oncol
A preliminary study on the safety and efficacy of 177Lu-FAP-2286 in gastrointestinal tumours with positive FAP expression. [Abstract]2025 Oct 4:213:111195. PMID: 41052603 -
Pharmaceuticals (Basel)
[68Ga]Ga-FAP-2286-Synthesis, Quality Control and Comparison with [18F]FDG PET/CT in a Patient with Suspected Cholangiocellular Carcinoma. [Abstract]2024 Aug 29;17(9):1141. PMID: 39338305
Rofapitide tetraxetan purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2024 Aug 29;17(9):1141. [Abstract]
MIP and hybrid PET/CT scan slice from December 2023 using [68Ga]Ga-FAP-2286 (Rofapitide tetraxetan): the red arrow marks an intense focal tracer uptake, which has been interpreted as the primary tumor lesion atop the confluence of the right and left hepatic bile ducts (Klatskin tumor). SUVmax 13.7; SUVpeak 10.7.
Rofapitide tetraxetan purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2024 Aug 29;17(9):1141. [Abstract]
MIP and hybrid PET/CT scan slice from March 2024 using [68Ga]Ga-FAP-2286 (Rofapitide tetraxetan): the red arrow marks the primary tumor lesion with an increasing size and tracer uptake at this time point after chemotherapy with cisplatin, gemcitabine, and durvalumab. SUVmax 24.6; SUVpeak 20.5.
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Bioorg Chem
Squaric-acid-engineered FAP2286: A next-generation 68Ga/177Lu theranostic ligand with synergistically enhanced affinity, hydrophilicity, and tumor retention. [Abstract]2025 Nov:166:109185. PMID: 41177127 -
Sci Rep
Preclinical evaluation of [13xLa]La-FAP-2286 as a novel theranostic agent for tumors expressing fibroblast activation protein. [Abstract]2025 Mar 3;15(1):7475. PMID: 40032959
Rofapitide tetraxetan purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Mar 3;15(1):7475. [Abstract]
Binding percentage of [13xLa]La-FAPI-2286 using HEK FAP+, and MCF7 and CHO FAP-cells.
Rofapitide tetraxetan purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Mar 3;15(1):7475. [Abstract]
Percentage of internalized [13xLa]La-FAPI-2286 to HEK cells overexpressed FAP receptors, and CHO cells, control cells, as a function of time.
Rofapitide tetraxetan purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Mar 3;15(1):7475. [Abstract]
The %ID/g of the normal mice up to 48 h post-injection of [13xLa]La-FAPI-2286. All values were presented as mean ± standard deviation (P value < 0.05).
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EJNMMI Res
Head-to-head comparison of [177Lu]Lu-FAP-2286 and [161Tb]Tb-FAP-2286 efficacy in a PDAC mouse model. [Abstract]2026 Jan 9;16(1):29. PMID: 41511675 -
Nucl Med Biol
Illuminating radionuclide therapy response: Monitoring cancer cell and CAF survival in a direct 2D co-culture model. [Abstract]2025 Oct 10:150-151:109571. PMID: 41108813 -
Solvent & Solubility
H2O : ≥ 100 mg/mL (67.99 mM)
DMSO : ≥ 50 mg/mL (34.00 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 (protect from light, 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (protect from light, 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: PBS
Solubility: 50 mg/mL (34.00 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (278 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
[2]. Richard P Baum, et al. Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using 177 Lu-FAP-2286: First-in-Humans Results. J Nucl Med. 2022 Mar;63(3):415-423. [Content Brief]
[3]. Zboralski D, Hoehne A, Bredenbeck A, et al. Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy. Eur J Nucl Med Mol Imaging. 2022;49(11):3651-3667. [Content Brief]
[4]. Pang Y, Zhao L, Meng T, et al. PET Imaging of Fibroblast Activation Protein in Various Types of Cancer Using 68Ga-FAP-2286: Comparison with 18F-FDG and 68Ga-FAPI-46 in a Single-Center, Prospective Study. J Nucl Med. 2023;64(3):386-394. [Content Brief]
[5]. Zboralski D, et al. Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy. Eur J Nucl Med Mol Imaging. 2022 Sep;49(11):3651-3667. [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 (protect from light, 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 |
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| DMSO / H2O | 1 mM | 0.6799 mL | 3.3996 mL | 6.7992 mL | 16.9979 mL |
| 5 mM | 0.1360 mL | 0.6799 mL | 1.3598 mL | 3.3996 mL | |
| 10 mM | 0.0680 mL | 0.3400 mL | 0.6799 mL | 1.6998 mL | |
| 15 mM | 0.0453 mL | 0.2266 mL | 0.4533 mL | 1.1332 mL | |
| 20 mM | 0.0340 mL | 0.1700 mL | 0.3400 mL | 0.8499 mL | |
| 25 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6799 mL | |
| 30 mM | 0.0227 mL | 0.1133 mL | 0.2266 mL | 0.5666 mL | |
| H2O | 40 mM | 0.0170 mL | 0.0850 mL | 0.1700 mL | 0.4249 mL |
| 50 mM | 0.0136 mL | 0.0680 mL | 0.1360 mL | 0.3400 mL | |
| 60 mM | 0.0113 mL | 0.0567 mL | 0.1133 mL | 0.2833 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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