2. Immunology/Inflammation
  3. FAP
  4. Rofapitide tetraxetan

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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CAS No. : 2581741-18-4

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
50 mg   Obtenir un devis  
100 mg   Obtenir un devis  

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Based on 7 publication(s) in Google Scholar

Other Forms of Rofapitide tetraxetan:

Rofapitide tetraxetan Related Antibodies

Top Publications Citing Use of Products

    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). SUVmax 13.7; SUVpeak 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. SUVmax 24.6; SUVpeak 20.5.

    • Activité biologique

    • Pureté et documentation

    • Références

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    Description

    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[1].

    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.

    Rofapitide tetraxetan Related Antibodies
    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.
    Masse moléculaire

    1470.77

    Formule

    C67H99N13O18S3
    CAS No.
    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
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage

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

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

    Solvant et solubilité
    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
    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.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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)

    g

    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).
    Pureté et documentation

    Purity: 99.54%

    SDS (252 KB)

    COA (255 KB) LCMS (87 KB)

    Instruction de manipulation (2659 KB)
    Références

    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.

    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.

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    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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