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Cat. No.: HY-147057A

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Rofapitide tetraxetan acetate

(Synonyms: FAP-2286 acetate)

7 Cited Publications

Customer Review

Based on 7 publication(s) in Google Scholar

Rofapitide tetraxetan (FAP-2286) acetate is a potent and selective FAP-binding peptide with a mean IC₅₀ value of 2.7 nM for binding to FAP. Rofapitide tetraxetan acetate can be labeled with radionuclides for diagnostic applications. Rofapitide tetraxetan acetate has antitumor activity.

For research use only. We do not sell to patients.

Formula: C₆₉H₁₀₃N₁₃O₂₀S₃
Molecular Weight:1530.83

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

Rofapitide tetraxetan acetate Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Clinical Trial
Chemical Information
Publications (7)
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

FAP^[1]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

Appearance Solid
Molecular Weight 1530.83
Formula C₆₉H₁₀₃N₁₃O₂₀S₃
Color White to off-white
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.CC(O)=O
Synonyms

FAP-2286 acetate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (7)

All Histological Imaging/StainingBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

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 acetate 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). SUV_max 13.7; SUV_peak 10.7.

Rofapitide tetraxetan acetate 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. SUV_max 24.6; SUV_peak 20.5.
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 acetate 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 acetate 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 acetate 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).
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
Res Sq

2025 Dec 22.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Baum RP, et al. Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using 177Lu-FAP-2286: First-in-Humans Results. J Nucl Med. 2022 Mar;63(3):415-423. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Rofapitide tetraxetan acetate

7 Cited Publications

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100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- Clinical Trial
Chemical Information
Publications (7)
Purity & Documentation
References

1/16
1/16

Rofapitide tetraxetan acetate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Mar 3;15(1):7475. [Abstract]

Customer Validation
Binding percentage of [^13xLa]La-FAPI-2286 using HEK FAP+, and MCF7 and CHO FAP-cells.
1/16

Rofapitide tetraxetan acetate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Mar 3;15(1):7475. [Abstract]

Customer Validation
Percentage of internalized [^13xLa]La-FAPI-2286 to HEK cells overexpressed FAP receptors, and CHO cells, control cells, as a function of time.
1/16

Rofapitide tetraxetan acetate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Mar 3;15(1):7475. [Abstract]

Customer Validation
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).
1/16

Rofapitide tetraxetan acetate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2024 Aug 29;17(9):1141. [Abstract]

Customer Validation
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). SUV_max 13.7; SUV_peak 10.7.
1/16

Rofapitide tetraxetan acetate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2024 Aug 29;17(9):1141. [Abstract]

Customer Validation
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. SUV_max 24.6; SUV_peak 20.5.

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Rofapitide tetraxetan acetate

Publications Citing Use of MedChemExpress (MCE) Rofapitide tetraxetan acetate

Biological Activity

Chemical Information

Publications (7)

Purity & Documentation

References

Calculators

Help & FAQs

Rofapitide tetraxetan acetate Related Classifications

Cat. No.: HY-147057A