FAP-2286 |
Catalog No.GC65537
One-Click Copy Product Info
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FAP-2286 is a potent and selective FAP-binding peptide conjugated to a radionuclide chelator with a mean IC50 value of 2.7 ± 0.9nM for inhibiting human FAP protease activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2581741-18-4
Sample solution is provided at 25 µL, 10mM.
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FAP-2286 is a potent and selective FAP-binding peptide conjugated to a radionuclide chelator with a mean IC50 value of 2.7 ± 0.9nM for inhibiting human FAP protease activity. Fibroblast activation protein (FAP) is a membrane-bound protease highly expressed on cancer-associated fibroblasts (CAFs) and some tumor cells, with limited expression in normal adult tissues. The high binding affinity FAP-2286 enables the attachment of radionuclides for imaging and therapeutic use in oncology[1][2].
In vitro, [13xLa]La-FAP-2286 (1-100nM) incubated HEK-FAP+ and CHO FAP- cells confirming the strong affinity of the radiolabeled complex to the FAPI-expressing human cell line[3].
In vivo, 177Lu-FAP-2286 (30 or 60MBq/nmol) was administrated into HEK-FAP xenograft mouse model via Intravenous injection. Signifcant antitumor activity was observed with tumor growth inhibition (TGI) of 111% and 113% respectively on day 14[1]. [13xLa]La-FAP-2286 (200µL, 7.4MBq) were intravenously (i.v.) injected into both normal and HEK FAP+ tumor-bearing mice through their tail vein. The biodistribution of [13xLa]La-FAP-2286 in tumor-bearing mice showed the significant accumulation of the radiolabeled compound in tumors and kidney[3]. FAP-2286-modified LNP-based nano vector (20mg/kg) was administered via intravenous injection in subcutaneous RM-1 tumor model. Tumor accumulation was significantly increased at each time point (3, 6, 9, 12, and 24 hours after injection), with 2.1-fold, 3.2-fold, 9.2-fold, and 10.5-fold increases, respectively camparing to unmodified LNP[4].
References:
[1] 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 Sep;49(11):3651-3667.
[2] Pang Y C, Zhao L, Meng T H, 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 Mar;64(3):386-394.
[3] Shirpour A, Hadadi A, Zolghadri S,et al. Preclinical evaluation of [13xLa]La-FAP-2286 as a novel theranostic agent for tumors expressing fibroblast activation protein. Sci Rep. 2025 Mar 3;15(1):7475.
[4] Qi F, Fu D, Cai H Z, et al. Metabolic Reprogramming of Cancer-Associated Fibroblasts: Transforming Tumor Accomplices into Immunotherapeutic Allies. Adv. Funct. Mater. 2024, 2418240
| Cell experiment [1]: | |
Cell lines | HEK FAP+ cells |
Preparation Method | Approximately one million HEK FAP+ cells were seeded into the wells of a 6-well plate along containing a complete culture medium and incubated for 24h. Then, the culture medium was removed, the cells were washed, and incubated with fresh culture medium for 1h at 37°C. The plates were then placed on ice for 30min, and different concentrations of FAP-2286 (1-100nM) were added. For internalization studies, the radiolabeled compound was incubated with cells for 30, 60, 120, 240, and 360min at 37˚C. |
Reaction Conditions | 1-100nM; 30, 60, 120, 240, and 360min |
Applications | The binding of [13xLa]La-FAP-2286 on HEK FAP + cell line was evaluated, demonstrating a dissociation constant (KD) value of 0.51 ± 0.12nM, confirming the strong affinity of the radiolabeled complex to the FAP-expressing human cell line. |
| Animal experiment [1]: | |
Animal models | NOD/SCID mice |
Preparation Method | [13xLa]La-FAP-2286 (200µL, 7.4MBq) were intravenously (i.v.) injected into both normal and tumor-bearing mice through their tail vein. 8–10-week-old NOD/SCID tumor-bearing mice with an average weight of 21.4±1.7 gr were used for biodistribution studies. Tumor induction was achieved by injecting approximately 1 million HEK FAP+cells subcutaneously into the mice’s flanks. |
Dosage form | 200µL, 7.4MBq; i.v.; one dose |
Applications | The biodistribution of FAP-2286 in tumor-bearing mice showed the significant accumulation of the radiolabeled compound in tumors at different time intervals. Also, a significant accumulation of activity was observed in the kidney after injection of the radiolabeled compound, which is related to the high hydrophilicity of the compound and its excretion via the urinary tract. |
References: | |
| Cas No. | 2581741-18-4 | SDF | |
| Formula | C67H99N13O18S3 | M.Wt | 1470.77 |
| Solubility | Water : ≥ 100 mg/mL (67.99 mM) | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 679.9 μL | 3.3996 mL | 6.7992 mL |
| 5 mM | 136 μL | 679.9 μL | 1.3598 mL |
| 10 mM | 68 μL | 340 μL | 679.9 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)