Rofapitide tetraxetan (Synonyms: FAP-2286)

Name: Rofapitide tetraxetan
Brand: MedChemExpress
SKU: HY-147057
Rating: 5.0 (7 reviews)

Cat. No.: HY-147057 Pureza: 99.54%: Ficha de datos
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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.

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No. CAS : 2581741-18-4

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
50 mg	Obtener un presupuesto
100 mg	Obtener un presupuesto

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Revisión del cliente

Based on 7 publication(s) in Google Scholar

Other Forms of Rofapitide tetraxetan:

3BP-4089 In-stock
Rofapitide tetraxetan acetate Obtener un presupuesto

7 Publications Citing Use of MCE Rofapitide tetraxetan

•Res Sq. 2025 Dec 22.

Histological Imaging/Staining

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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).

: Rofapitide tetraxetan 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 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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Referencias
Revisión del cliente

Descripciòn

In Vitro

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.

In Vivo

Rofapitide tetraxetan (30 MBq/nmol for intravenous injection) accumulated atably maintained in the tumors of HEK-FAP tumor-bearing mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	HEK-FAP tumor-bearing mice^[1]
Dosage:	30 MBq/nmol
Administration:	Intravenous injection (i.v.)
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.

Peso molecular

1470.77

Fòrmula

C₆₇H₉₉N₁₃O₁₈S₃

No. CAS

2581741-18-4

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvente y solubilidad

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.6799 mL	3.3996 mL	6.7992 mL
5 mM	0.1360 mL	0.6799 mL	1.3598 mL
10 mM	0.0680 mL	0.3400 mL	0.6799 mL

View the 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.

* 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (34.00 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Pureza y Documentación

Purity: 99.54%

Select Batch:

Ficha de datos (278 KB) SDS (252 KB)

COA (255 KB) LCMS (87 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Dirk Zboralski, et al. Comparative Biodistribution and Radiotherapeutic Efficacy of the Fibroblast Activation Protein (FAP)–Targeting Agents FAP-2286 and FAPI-46.

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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.

Rofapitide tetraxetan Related Classifications

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 tetraxetan2581741-18-4FAP-2286FAP2286FAP 2286FAPFibroblast activation proteintheranostictumorpepetide-targetedradionuclides therapyInhibitorinhibitorinhibit

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Rofapitide tetraxetan (Synonyms: FAP-2286)

Revisión del cliente

Other Forms of Rofapitide tetraxetan:

Rofapitide tetraxetan Related Antibodies

7 Publications Citing Use of MCE Rofapitide tetraxetan

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Rofapitide tetraxetan Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Rofapitide tetraxetan Related Classifications

Keywords:

Productos vistos recientemente:

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