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FAPI-X5

Name: FAPI-X5
Brand: TargetMol
SKU: T217935
Rating: 4.5 (1 reviews)

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FAPI-X5 is an inhibitor of fibroblast activation protein (FAP). It binds to the catalytic domain of FAP, forming hydrogen bonds and engaging in π-π stacking with key active residues, resulting in functional inhibition. FAPI-X5 exhibits albumin-binding activity, which extends its systemic circulation half-life. It shows cytostatic effects on glioblastoma cells, slowing tumor growth without causing tumor regression. When labeled with [^68Ga], FAPI-X5 serves as a PET tracer, displaying rapid tumor uptake and high-contrast imaging in glioblastoma-bearing mice. Additionally, when labeled with [^177Lu] or [^47Sc], it acts as a targeted radionuclide therapeutic, offering prolonged tumor retention. FAPI-X5 is applicable in glioblastoma research.

FAPI-X5

Cas No. 3056070-96-0

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	FAPI-X5 is an inhibitor of fibroblast activation protein (FAP). It binds to the catalytic domain of FAP, forming hydrogen bonds and engaging in π-π stacking with key active residues, resulting in functional inhibition. FAPI-X5 exhibits albumin-binding activity, which extends its systemic circulation half-life. It shows cytostatic effects on glioblastoma cells, slowing tumor growth without causing tumor regression. When labeled with [^68Ga], FAPI-X5 serves as a PET tracer, displaying rapid tumor uptake and high-contrast imaging in glioblastoma-bearing mice. Additionally, when labeled with [^177Lu] or [^47Sc], it acts as a targeted radionuclide therapeutic, offering prolonged tumor retention. FAPI-X5 is applicable in glioblastoma research.
In vitro	FAPI-X5 (10 μg), when radiolabeled with [68 Ga], [177 Lu], or [47 Sc], demonstrates a radiochemical purity of over 95%, an albumin binding rate exceeding 40%, and good stability in vitro. Among these, [68 Ga-FAPI-X5] is the most hydrophilic, while [177 Lu-] and [47 Sc-FAPI-X5] show slightly higher albumin binding rates. For FAPI-X5 (30-240 min), after radiolabeling with [68 Ga], [177 Lu], or [47 Sc], there is time-dependent cellular uptake in FAP-expressing U87MG cells, with the uptake of [68 Ga-FAPI-X5] peaking at 2 hours and all labeled variants reaching their highest uptake by 4 hours.
In vivo	FAPI-X5 (177 Lu-FAPI-X5 and 47 Sc-FAPI-X5) [18.5-55.5 MBq; intravenous injection; single dose] induces a cell inhibitory effect in U87MG glioblastoma-bearing mice (T/C value of 35.49%-57.2%), but is associated with dose-dependent hepatogastrointestinal toxicity.

Chemical Properties

Molecular Weight	1428.37
Formula	C₆₃H₈₈F₂IN₁₅O₁₃
Cas No.	3056070-96-0
Smiles	C(NCC(=O)N1[C@H](C#N)CC(F)(F)C1)(=O)C=2C3=C(C=CC(OCCCC4CCN(C([C@@H](NC([C@@H](NC(CCCC5=CC=C(I)C=C5)=O)CCCCNC(CN6CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC6)=O)=O)CCCNC(=N)N)=O)CC4)=C3)N=CC2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Related Tags: FAPI-X5 in vivo | FAPI-X5 in vitro | FAPI-X5 formula | FAPI-X5 molecular weight