Rofapitide tetraxetan acetate (Synonyms: FAP-2286 acetate)

Cat. No.: HY-147057A: Data Sheet
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Handling Instructions
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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.

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Other In-stock Forms of Rofapitide tetraxetan acetate:

Rofapitide tetraxetan

Other Forms of Rofapitide tetraxetan acetate:

Rofapitide tetraxetan In-stock

7 Publications Citing Use of MCE Rofapitide tetraxetan acetate

•Res Sq. 2025 Dec 22.

Histological Imaging/Staining

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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).

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

IC₅₀ & Target

FAP^[1]

Clinical Trial

Molecular Weight

1530.83

Formula

C₆₉H₁₀₃N₁₃O₂₀S₃

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Data Sheet (272 KB) SDS (252 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]

Rofapitide tetraxetan acetate Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rofapitide tetraxetanFAP-2286FAP2286FAP 2286FAPFibroblast activation proteinAntitumorfibroblast activation proteinInhibitorinhibitorinhibit

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