2. Immunology/Inflammation
  3. FAP
  4. FAPI-4

FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.

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

FAPI-4 Chemical Structure

FAPI-4 Chemical Structure

CAS No. : 2374782-02-0

Size Price Stock Quantity
5 mg USD 780 In-stock
10 mg USD 1250 In-stock
25 mg USD 2550 In-stock
50 mg USD 3950 In-stock
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Based on 21 publication(s) in Google Scholar

FAPI-4 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios[1][2].

IC50 & Target

Fibroblast activation protein (FAP)[1]
In Vivo

FAPI-4 (Intravenous injection; 30 nmol per mouse; once) shows excellent tumor uptake in BALB/c nu/nu mice[2].

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

Animal Model: 8-week-old BALB/c nu/nu mice inoculated with HT-1080-FAP cells[2]
Dosage: 30 nmol per mouse
Administration: Intravenous injection; 30 nmol per mouse; once
Result: Revealed the high overall tumor uptake (9.44%ID/g 4 h after injection).
Molecular Weight

872.91

Formula

C40H54F2N10O10
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC(N1CC(F)(F)C[C@]1(C#N)[H])=O)C2=CC=NC3=CC=C(OCCCN4CCN(C(CN5CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC5)=O)CC4)C=C32
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (114.56 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 1.1456 mL 5.7280 mL 11.4559 mL
5 mM 0.2291 mL 1.1456 mL 2.2912 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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:

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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:  Saline

    Solubility: 4 mg/mL (4.58 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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.42%

COA (248 KB) HNMR (265 KB) LCMS (138 KB)

Handling Instructions (2659 KB)
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 (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 1 mM 1.1456 mL 5.7280 mL 11.4559 mL 28.6398 mL
5 mM 0.2291 mL 1.1456 mL 2.2912 mL 5.7280 mL
10 mM 0.1146 mL 0.5728 mL 1.1456 mL 2.8640 mL
15 mM 0.0764 mL 0.3819 mL 0.7637 mL 1.9093 mL
20 mM 0.0573 mL 0.2864 mL 0.5728 mL 1.4320 mL
25 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1456 mL
30 mM 0.0382 mL 0.1909 mL 0.3819 mL 0.9547 mL
40 mM 0.0286 mL 0.1432 mL 0.2864 mL 0.7160 mL
50 mM 0.0229 mL 0.1146 mL 0.2291 mL 0.5728 mL
60 mM 0.0191 mL 0.0955 mL 0.1909 mL 0.4773 mL
80 mM 0.0143 mL 0.0716 mL 0.1432 mL 0.3580 mL
100 mM 0.0115 mL 0.0573 mL 0.1146 mL 0.2864 mL
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FAPI-4 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:

FAPI-42374782-02-0FAPI4FAPI 4FAPFibroblast activation proteinradiotracer tissue kineticscancer-associated fibroblastsPET/CTbiodistributiondosimetryfibroblast activation proteinInhibitorinhibitorinhibit

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