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| 5mg |
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| Targets |
FT-FAPI-12_9 targets Fibroblast Activation Protein (FAP), a serine protease that is highly expressed on the surface of cancer-associated fibroblasts (CAFs) in various solid tumors, but is largely absent from normal adult tissues. It functions as a FAP-binding moiety, where its structure is specifically designed to bind with high affinity to the active site of FAP. This property makes it a key building block for imaging and therapeutic conjugates.
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| ln Vitro |
In non-cell biochemical assays, FT-FAPI-12_9 is not typically tested for direct activity. Its high-affinity binding to FAP is evaluated after it is conjugated into a radiotracer, such as FAPI-46. The binding affinity (KD) of the resulting radiotracer for the FAP protein is measured using surface plasmon resonance (SPR) or saturation binding assays on FAP-expressing cell membranes, confirming its high specificity and affinity.
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| ln Vivo |
No direct in vitro cell-based activity for FT-FAPI-12_9 alone is available. The activity is assessed using its derivative, FAPI-46. In a typical cell-based assay, FAP-expressing cancer-associated fibroblasts (CAFs) are incubated with the radiolabeled FAPI-46 tracer. High cellular uptake, which can be blocked by an excess of unlabeled tracer, confirms specific and high-affinity binding to the FAP protein on the cell surface.
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| Enzyme Assay |
As FT-FAPI-12_9 is a precursor for radiotracer synthesis, no in vivo studies are performed with the compound itself. The in vivo behavior is characterized using its radiolabeled conjugate, FAPI-46. In mouse xenograft models of human cancers (e.g., pancreatic, breast), intravenous injection of [⁶⁸Ga]Ga-FAPI-46 results in rapid and high tumor uptake with low background, as visualized by PET/CT imaging, confirming its excellent in vivo targeting properties and potential for diagnostic imaging.
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| Cell Assay |
For non-cell experiments, the binding affinity of the FAPI-46 radiotracer for FAP can be determined. Recombinant human FAP protein is immobilized on a sensor chip. Increasing concentrations of FAPI-46 are flowed over the chip. The binding kinetics are recorded, and the dissociation constant (KD) is calculated. High-affinity binding, typically in the low nanomolar range, confirms the high specificity of the conjugate derived from FT-FAPI-12_9.
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| Animal Protocol |
No cell-based assays are performed directly with FT-FAPI-12_9. For in vitro studies, FAP-positive cells (e.g., HEK293:FAP or U87MG cells) are seeded in 12-well plates. The cells are then incubated with the radiolabeled FAPI-46 tracer (e.g., [⁶⁸Ga]Ga-FAPI-46) in binding buffer. After a 60-minute incubation at 37degC, the cells are washed and lysed, and the bound radioactivity is measured in a gamma counter. Specific binding is confirmed by co-incubation with an excess of unlabeled FAPI-46.
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| ADME/Pharmacokinetics |
No direct in vivo animal study data is available for FT-FAPI-12_9. For in vivo imaging studies, the radiolabeled derivative [⁶⁸Ga]Ga-FAPI-46 is used. BALB/c nude mice bearing subcutaneous FAP-expressing tumor xenografts (e.g., HEK293:FAP) are injected intravenously with the radiotracer. At 60 minutes post-injection, the mice are imaged using a PET/CT scanner. High-contrast tumor visualization confirms the excellent in vivo targeting properties of the FAPI ligand derived from FT-FAPI-12_9.
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| Toxicity/Toxicokinetics |
Pharmacokinetic data for FT-FAPI-12_9 alone is not available. The pharmacokinetic properties of its derivative, FAPI-46, are well-characterized for imaging applications. It is rapidly cleared from the bloodstream, leading to high tumor-to-background ratios. For research use, FT-FAPI-12_9 is stored as a powder at -20degC for long-term stability. It is soluble in DMSO, where stock solutions can be prepared and stored at -80degC.
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| References | |
| Additional Infomation |
Toxicity data for FT-FAPI-12_9 is not available. As a research chemical, it should be handled with caution. The compound is intended for research use only, not for human or veterinary use. Standard safety practices for handling chemical substances should be followed, including the use of PPE (gloves, lab coat, safety goggles) and working in a well-ventilated area.
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| Molecular Formula |
C25H31F2N7O2
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|---|---|
| Molecular Weight |
499.56
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| CAS # |
2883407-81-4
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| Appearance |
Light yellow to yellow solid powder
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| SMILES |
FC1(CN(C(CNC(C2C=CN=C3C=CC(=CC=23)N(C)CCCN2CCNCC2)=O)=O)[C@H](C#N)C1)F
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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 |
| 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) |
DMSO : ~125 mg/mL (~250.22 mM; with heating and sonication)
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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 | 2.0018 mL | 10.0088 mL | 20.0176 mL | |
| 5 mM | 0.4004 mL | 2.0018 mL | 4.0035 mL | |
| 10 mM | 0.2002 mL | 1.0009 mL | 2.0018 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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