1. Immunology/Inflammation
  2. FAP
  3. FAPI-46

FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted tracer. Use radioactivity FAPI-46 labeled with 68Ga or 177Lu can be used for tumor imaging in a variety of cancers and has higher tumor uptake rates and longer tumor accumulation.

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

CAS No. : 2374782-04-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    FAPI-46 purchased from MedChemExpress. Usage Cited in: Nucl Med Biol. 2025 Oct 10:150-151:109571.  [Abstract]

    Radiotracer uptake studies in the applied cell lines. Specific uptake of 1 nM [111In]In-FAPI-46 by PS-1-CBG99-RFP (n = 4), Panc-1-CBR2-GFP (n = 2), 19T-TF-CBG99-RFP (n = 3), and T47D-CBR2-GFP (n = 2). %AA = percentage added dose, BC = breast cancer, PDAC = pancreatic ductal adenocarcinoma.

    FAPI-46 purchased from MedChemExpress. Usage Cited in: Appl Radiat Isot. 2024 Apr:206:111211.  [Abstract]

    Mean RCP and RCY values obtained by TLC and HPLC during the study of the influence of the reaction buffer on the radiolabeling of [68Ga]Ga-FAPI-46.

    FAPI-46 purchased from MedChemExpress. Usage Cited in: Appl Radiat Isot. 2024 Apr:206:111211.  [Abstract]

    Radio-TLC spectra of [68Ga]Ga-FAPI-46 after radiolabeling with HEPES 0.3 M or with HEPES 0.3 M + gentisic acid 0.6 mg/mL and elution of the TLC plate with aqueous 0.1 M sodium citrate pH 5 or with aqueous 1 M ammonium acetate in methanol (1:1).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted tracer. Use radioactivity FAPI-46 labeled with 68Ga or 177Lu can be used for tumor imaging in a variety of cancers and has higher tumor uptake rates and longer tumor accumulation[1][2].

    IC50 & Target

    fibroblast activation protein (FAP)[1]

    In Vitro

    FAPI-46 (1-24 h) robustly binds to human FAP in human FAP-expressing HT-1080 cells[1].

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

    In Vivo

    FAPI-46 (i.v.) shows improved ratios of tumor to liver, kidney, and brain uptake, resulting in an enhanced image contrast for PET imaging[1].

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

    Clinical Trial
    Molecular Weight

    885.96

    Formula

    C41H57F2N11O9

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=CC=NC(C=C2)=C1C=C2N(C)CCCN(CC3)CCN3C(CN(CCN(CC4)CC(O)=O)CCN(CCN4CC(O)=O)CC(O)=O)=O)NCC(N(CC5(F)F)[C@@H](C5)C#N)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (112.87 mM; Need ultrasonic)

    DMSO : 100 mg/mL (112.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1287 mL 5.6436 mL 11.2872 mL
    5 mM 0.2257 mL 1.1287 mL 2.2574 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 (sealed storage, away from moisture). 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5.75 mg/mL (6.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (5.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    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).
    Purity & Documentation

    Purity: 99.02%

    References

    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 (sealed storage, away from moisture). 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
    H2O / DMSO 1 mM 1.1287 mL 5.6436 mL 11.2872 mL 28.2180 mL
    5 mM 0.2257 mL 1.1287 mL 2.2574 mL 5.6436 mL
    10 mM 0.1129 mL 0.5644 mL 1.1287 mL 2.8218 mL
    15 mM 0.0752 mL 0.3762 mL 0.7525 mL 1.8812 mL
    20 mM 0.0564 mL 0.2822 mL 0.5644 mL 1.4109 mL
    25 mM 0.0451 mL 0.2257 mL 0.4515 mL 1.1287 mL
    30 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.9406 mL
    40 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7054 mL
    50 mM 0.0226 mL 0.1129 mL 0.2257 mL 0.5644 mL
    60 mM 0.0188 mL 0.0941 mL 0.1881 mL 0.4703 mL
    80 mM 0.0141 mL 0.0705 mL 0.1411 mL 0.3527 mL
    100 mM 0.0113 mL 0.0564 mL 0.1129 mL 0.2822 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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    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.

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    Product Name:
    FAPI-46
    Cat. No.:
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