| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
This compound targets fibroblast activation protein (FAP), a 170 kDa type II transmembrane serine protease expressed at high levels by CAFs in over 90% of epithelial cancers including breast, lung, colon, pancreatic, and ovarian carcinomas. FAP has both dipeptidyl peptidase and endopeptidase activities and is involved in extracellular matrix remodeling and tumor progression.
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| ln Vitro |
FAP-IN-2 TFA functions by binding with high affinity to FAP expressed on the surface of CAFs. The 99mTc radiolabel enables single-photon emission computed tomography (SPECT) imaging after systemic administration, allowing non-invasive visualization of FAP expression in tumors. Its isonitrile chelating group stabilizes the technetium-99m complex.
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| ln Vivo |
The compound is used in animal models to evaluate tumor targeting and biodistribution for SPECT imaging. In vivo, it specifically accumulates in FAP-positive tumors with favorable tumor-to-background ratios, enabling sensitive detection of primary and metastatic lesions. The TFA salt form ensures high solubility and stability for radiolabeling and injection.
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| Enzyme Assay |
For radiolabeling: dissolve FAP-IN-2 in 0.1 M phosphate buffer (pH 7-8), add 99mTc-pertechnetate (eluted from a 99Mo/99mTc generator) and a reducing agent (SnCl2·2H2O) to reduce Tc(VII) to Tc(V). Heat at 100degC for 15-20 minutes. Purify by C18 Sep-Pak cartridge. Assess radiolabeling efficiency by thin-layer chromatography or radio-HPLC (target >95% radiochemical purity).
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| Cell Assay |
Not applicable as FAP-IN-2 TFA is a radiotracer for imaging rather than a drug for cellular assays. However, for FAP binding confirmation, incubate FAP-expressing cell lines (e.g., HT-1080 human fibrosarcoma cells) with increasing concentrations of unlabeled FAP-IN-2 (1 nM-10 uM) for 1-2 hours at 4degC, followed by fluorescence or radiolabeled FAP ligand competition to determine IC50. For uptake studies, treat cells with 99mTc-labeled FAP-IN-2 and measure cell-associated radioactivity.
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| Animal Protocol |
For tumor imaging studies, use FAP-positive tumor-bearing mouse models (e.g., subcutaneous or orthotopic xenografts of HT-1080, U87MG, or patient-derived CAF-rich tumors). Administer 50-200 uCi (approximately 10-50 ug) of 99mTc-FAP-IN-2 TFA via intravenous (tail vein) injection. Perform SPECT/CT imaging at various time points (30 min, 1, 2, 4, 6, 24 h post-injection) to assess tumor uptake, retention, and biodistribution. After imaging, harvest major organs and tumor for gamma counting to quantify %ID/g tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic evaluation is primarily focused on radiotracer properties. The 99mTc-labeled compound is expected to have rapid blood clearance with renal elimination, as is typical for small hydrophilic radiopharmaceuticals. Maximum tumor uptake is generally achieved within 1-2 hours post-injection. The TFA salt improves water solubility, enhancing bioavailability for intravenous administration.
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| Toxicity/Toxicokinetics |
The toxicological profile is consistent with other 99mTc-labeled radiopharmaceuticals at diagnostic doses, having negligible mass toxicity due to the very small amount of compound administered (microgram quantities). The primary toxicity concern relates to radiation exposure; however, 99mTc has a short half-life (6 hours) and low radiation dose, making it safe for diagnostic imaging. No specific toxicity data are available for the non-radioactive compound.
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| References | |
| Additional Infomation |
FAP-IN-2 TFA is covered under patent CN112409414A for preparation methods of technetium-99m-labeled isocyanide-containing FAP inhibitor derivatives. Compared to FAPI-2 (which uses 68Ga for PET imaging), FAP-IN-2 uses 99mTc for SPECT imaging, which has advantages in cost and availability for routine clinical use. The compound is exclusively for research use and not for human diagnostic applications.
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| Molecular Formula |
C26H29F5N6O5
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| Molecular Weight |
600.54
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| Related CAS # |
FAP-IN-2;2471983-20-5
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| Appearance |
Light yellow to yellow 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: 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) |
DMSO :~250 mg/mL (~416.29 mM)
H2O :~125 mg/mL (~208.15 mM) |
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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 | 1.6652 mL | 8.3258 mL | 16.6517 mL | |
| 5 mM | 0.3330 mL | 1.6652 mL | 3.3303 mL | |
| 10 mM | 0.1665 mL | 0.8326 mL | 1.6652 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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