| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
FT-FAPI-12_9 TFA functions as a ligand for Fibroblast Activation Protein (FAP), a membrane-bound serine protease that is selectively overexpressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment [6L4-L5, L11-L12, L14-L15]. By binding to FAP, this conjugate can deliver diagnostic isotopes (e.g., for PET imaging) or therapeutic radionuclides to FAP-expressing CAFs, enabling the visualization and treatment of various solid tumors.
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| ln Vitro |
FT-FAPI-12_9 TFA is used as a chemical building block to synthesize FAPI-46, a high-affinity FAP-targeted radiotracer. The biological activity of FAPI-46, which includes high specificity and nanomolar affinity for FAP, has been well characterized in vitro. This conjugate enables the development of imaging agents that can detect FAP-expressing CAFs with high contrast, making it valuable for tumor imaging and theranostic applications.
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| ln Vivo |
FAPI-46, synthesized using FT-FAPI-12_9 TFA, has been validated in vivo in preclinical studies and has advanced to clinical applications. In mouse xenograft models, FAPI-46 labeled with gallium-68 or other PET isotopes shows rapid and specific accumulation in FAP-positive tumors with high target-to-background ratios. The tracer also demonstrates fast clearance from non-target tissues, enabling high-contrast PET imaging within 1-3 hours post-injection, which is clinically advantageous for cancer diagnosis.
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| Enzyme Assay |
The assay is performed with the final FAP-targeted radiotracer, not the ligand precursor. To confirm FAP binding affinity, an enzyme inhibition assay can be used: Recombinant human FAP protein is incubated with varying concentrations of FAPI-46 in assay buffer containing a fluorogenic substrate (e.g., Ala-Pro-AMC). The release of fluorescent AMC is measured over time (excitation 380 nm, emission 460 nm). The IC50 value is calculated by plotting percent FAP inhibition versus log inhibitor concentration. Alternatively, surface plasmon resonance (SPR) can directly measure binding affinity (Kd).
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| Cell Assay |
The cellular activity is evaluated using the final FAP-targeted radiotracer. Procedure: FAP-positive (e.g., HT-1080 cells transfected with FAP) and FAP-negative control cells are seeded in 24-well plates and cultured to 80-90% confluence. Cells are incubated with 1-10 nM of radiolabeled FAPI-46 (e.g., [68Ga]Ga-FAPI-46) for 1 hour at 37degC. After incubation, cells are washed three times with cold PBS to remove unbound tracer. Cells are lysed, and cell-associated radioactivity is measured using a gamma counter. Specific binding is calculated by subtracting binding in the presence of excess unlabeled FAPI-46.
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| Animal Protocol |
Animal studies are performed with the final FAP-targeted radiotracer synthesized from FT-FAPI-12_9 TFA. Procedure: 6-8 week old female BALB/c nude mice are inoculated subcutaneously with FAP-positive HT-1080 cells. When tumors reach 200-300 mm3, mice receive an intravenous injection of 100-200 microCi (3.7-7.4 MBq) of [68Ga]Ga-FAPI-46 via tail vein. Dynamic PET/CT images are acquired for 60-120 minutes post-injection. At 60 minutes post-injection, mice are euthanized, and major organs are collected for biodistribution analysis. Radioactivity is measured in a gamma counter and expressed as %ID/g.
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| ADME/Pharmacokinetics |
PK properties are determined for the radiotracer (e.g., FAPI-46) rather than the ligand precursor. FAPI-46 radiotracers demonstrate favorable PK for imaging. They typically show rapid blood clearance (t1/2 of 10-20 minutes), low non-specific tissue retention, and high tumor uptake (typically 2-10% ID/g at 1 hour). Excretion is predominantly renal, with minimal hepatobiliary excretion. The fast clearance kinetics enable same-day imaging and low radiation dose to patients, which is a key advantage of FAPI-based radiotracers compared to FDG or other agents.
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| Toxicity/Toxicokinetics |
Specific toxicology data for FT-FAPI-12_9 TFA itself is not available. As a chemical precursor for radiotracer synthesis, its own toxicity profile is less relevant. The final radiolabeled product (e.g., [68Ga]Ga-FAPI-46) has been studied for toxicity. Preclinical safety studies indicate that FAPI-46 radiotracers are well-tolerated at diagnostic doses, with no observed acute toxicity in animal models at up to 1000 times the human-equivalent dose. No significant adverse effects have been reported in human studies.
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| References | |
| Additional Infomation |
FT-FAPI-12_9 TFA is an FAP ligand that serves as a key building block for the synthesis of the emerging class of FAP-targeted radiopharmaceuticals (FAPIs), particularly FAPI-46 [6L5, L7, L26-L27]. FAPI-based imaging agents are rapidly gaining recognition in nuclear oncology as promising alternatives to [18F]FDG for PET imaging of various cancers, especially those with low FDG avidity (e.g., sarcomas, peritoneal carcinomatosis, certain adenocarcinomas). The TFA salt form improves solubility and handling during the conjugation and radiolabeling process. This compound is strictly for research use and is not an FDA-approved drug for human use. FAP-targeted theranostics (combining imaging and therapy) using lutetium-177 or other therapeutic isotopes is an area of active preclinical and clinical investigation.
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| Molecular Formula |
C27H32F5N7O4
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| Molecular Weight |
613.58
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| Appearance |
Orange to red solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6298 mL | 8.1489 mL | 16.2978 mL | |
| 5 mM | 0.3260 mL | 1.6298 mL | 3.2596 mL | |
| 10 mM | 0.1630 mL | 0.8149 mL | 1.6298 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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