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Rofapitide tetraxetan
🥰Excellent
Catalog No. T74546Cas 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.
Rofapitide tetraxetan
🥰Excellent
Purity: 95.46%
Catalog No. T74546Cas 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 | Availability | 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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Purity:95.46%
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Product Introduction
Bioactivity
Chemical Properties
| 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. |
| 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 |
| Color | White |
| Appearance | Solid |
Storage & Solubility Information
| 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 |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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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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