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Rofapitide tetraxetan
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Catalog No. T74546Cas No. 2581741-18-4
Alias FAP-2286
Rofapitide tetraxetan (FAP-2286) is a high-affinity, selective inhibitor of fibroblast activating protein (FAP) and a DOTA-pseudopeptide with an IC₅₀ of 1.3–2.2 nM. FAP-2286 targets the tumour microenvironment and can be radiolabelled (e.g., with ⁶⁸Ga) for use in positron emission tomography (PET) imaging.
Rofapitide tetraxetan
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Purity: 95.46%
Catalog No. T74546Alias FAP-2286Cas No. 2581741-18-4
Rofapitide tetraxetan (FAP-2286) is a high-affinity, selective inhibitor of fibroblast activating protein (FAP) and a DOTA-pseudopeptide with an IC₅₀ of 1.3–2.2 nM. FAP-2286 targets the tumour microenvironment and can be radiolabelled (e.g., with ⁶⁸Ga) for use in positron emission tomography (PET) imaging.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $596 | - | In Stock | |
| 5 mg | $1,290 | - | In Stock | |
| 10 mg | $1,730 | - | In Stock | |
| 25 mg | $2,580 | - | In Stock | |
| 50 mg | $3,490 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:95.46%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Rofapitide tetraxetan (FAP-2286) is a high-affinity, selective inhibitor of fibroblast activating protein (FAP) and a DOTA-pseudopeptide with an IC₅₀ of 1.3–2.2 nM. FAP-2286 targets the tumour microenvironment and can be radiolabelled (e.g., with ⁶⁸Ga) for use in positron emission tomography (PET) imaging. |
| Targets&IC50 | FAP:2.7 nM |
| In vitro | Rofapitide tetraxetan exhibits high affinity for recombinant homo sapiens-derived and murine-derived FAP (KD values ranging between 0.2-4.7 nM) and demonstrates high selectivity in cell-based binding assays. |
| In vivo | Methods: 177Lu-Rofapitide tetraxetan (30MBq/nmol, single dose) was intravenously injected into HEK-FAP tumor-bearing mice, with tumor volume and body weight changes monitored to evaluate the anti-tumor efficacy of Rofapitide tetraxetan. Results: 177Lu-Rofapitide tetraxetan demonstrated significant anti-tumor activity, markedly reducing tumor volume without causing significant body weight loss. |
| Synonyms | FAP-2286 |
| Molecular Weight | 1470.77 |
| Formula | C67H99N13O18S3 |
| Cas No. | 2581741-18-4 |
| Smiles | [H][C@@]12CCCN1C(=O)[C@]1([H])CCCN1C(=O)[C@H](CSCc1cc(CSCCNC(=O)CN3CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC3)cc(CSC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@]([H])(NC2=O)[C@@H](C)O)C(O)=O)c1)NC(=O)CCCCC |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO: ≥ 40 mg/mL H2O: ≥ 80 mg/mL |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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