| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The compound targets the fibroblast activation protein (FAP), a serine protease that is highly overexpressed on cancer-associated fibroblasts (CAFs) in many solid tumors, including pancreatic, breast, lung, and colorectal cancers. FAP is involved in extracellular matrix remodeling and tumor progression. By inhibiting FAP, especially as a dimeric inhibitor, DOTAGA.(SA.FAPi)2 TFA binds with high affinity and selectivity, allowing for precise delivery of radionuclides to the tumor microenvironment for imaging or therapy.
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| ln Vitro |
As a dimeric FAP inhibitor, this compound exhibits high affinity for the FAP protein due to avidity effects. The DOTAGA chelator can form stable complexes with radiometals such as gallium-68 (for PET imaging) or lutetium-177 (for radionuclide therapy). The compound has the potential for use in cancer diagnostic research. Specific IC50 values are not provided, but the dimeric design enhances binding compared to monomeric FAP inhibitors.
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| ln Vivo |
The 68Ga- or 177Lu-labeled version of DOTAGA.(SA.FAPi)2 has been studied in preclinical models for theranostic applications. Labeled with gallium-68, it can be used for PET imaging of FAP-expressing tumors. Labeled with lutetium-177, it has potential for targeted radionuclide therapy. The compound is designed to deliver diagnostic or therapeutic radionuclides specifically to the tumor microenvironment, reducing off-target effects.
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| Enzyme Assay |
The binding affinity of DOTAGA.(SA.FAPi)2 TFA to FAP can be measured using a radioligand binding assay. Procedure: Membranes from FAP-expressing cells (e.g., HEK293-FAP) are incubated with 0.1 nM [125I]-FAPI-04 and varying concentrations of DOTAGA.(SA.FAPi)2 TFA (0.01-1000 nM) in binding buffer (50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) for 60 minutes at 25degC. Non-specific binding is determined with 1 uM unlabeled FAPI-04. Bound radioligand is separated by filtration through GF/B filters and counted. The Ki is calculated from the IC50 using the Cheng-Prusoff equation.
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| Cell Assay |
Cellular uptake of radiolabeled DOTAGA.(SA.FAPi)2 can be assessed in FAP-positive cells. Procedure: FAP-positive (e.g., HT-1080-FAP) and FAP-negative control cells are seeded in 12-well plates (2x10⁵ cells/well). The compound is labeled with 68Ga or 177Lu. Cells are incubated with 10 nM of the radiolabeled compound for 0.5-4 hours at 37degC. Cells are washed, lysed, and counted in a gamma counter. Specific binding is calculated as the difference between total binding and binding in the presence of excess unlabeled compound (10 uM). High uptake in FAP-positive cells and low uptake in FAP-negative cells indicates specificity.
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| Animal Protocol |
In vivo PET imaging can be performed in a mouse xenograft model of FAP-expressing tumors. Procedure: Female BALB/c nude mice are inoculated subcutaneously with 5x10⁶ FAP-positive HT-1080-FAP cells. When tumors reach 200-300 mm3, mice are injected intravenously with 100-200 uCi of 68Ga-labeled DOTAGA.(SA.FAPi)2. PET/CT images are acquired at 30, 60, and 120 minutes post-injection. Biodistribution is confirmed by harvesting organs at 60 minutes and counting in a gamma counter. High tumor uptake and low non-target organ uptake indicate that the compound is a promising FAP-targeted probe.
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| ADME/Pharmacokinetics |
The labeled compound exhibits rapid clearance and high tumor-to-background ratios. As a small molecule (approximately 1.6 kDa), it has a short circulation half-life and is cleared renally. The DOTAGA chelator forms stable complexes with radiometals, preventing in vivo transchelation. The TFA salt form enhances solubility for formulation. PK parameters depend on the specific radionuclide used.
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| Toxicity/Toxicokinetics |
Specific toxicology data for DOTAGA.(SA.FAPi)2 TFA is not provided. As a FAP-targeted probe, it is designed to deliver radionuclides specifically to tumors, minimizing systemic toxicity. The compound has been used in preclinical theranostic studies with acceptable tolerability. It is for research use only and is not an approved drug. Standard safety precautions for handling radiochemicals should be followed.
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| References | |
| Additional Infomation |
DOTAGA.(SA.FAPi)2 TFA is a potent dimeric FAP inhibitor for theranostic applications. Fibroblast activation protein (FAP) is overexpressed on cancer-associated fibroblasts in many solid tumors. The DOTAGA chelator allows for radiolabeling with 68Ga for PET imaging or 177Lu for radionuclide therapy. The dimeric design enhances avidity and binding affinity compared to monomeric FAP inhibitors. This compound has the potential for use in cancer diagnostic research. It is for research use only.
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| Molecular Formula |
C73H84F7N17O19
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|---|---|
| Molecular Weight |
1636.54
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| Appearance |
Typically exists as solids at room temperature
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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 | 0.6110 mL | 3.0552 mL | 6.1105 mL | |
| 5 mM | 0.1222 mL | 0.6110 mL | 1.2221 mL | |
| 10 mM | 0.0611 mL | 0.3055 mL | 0.6110 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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