| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Fibroblast activation protein (FAP), a cell-surface serine protease highly expressed in cancer-associated fibroblasts (CAFs) in over 90% of epithelial carcinomas, but minimally expressed in normal adult tissues. FAP is involved in tumor growth, invasion, and metastasis.
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| ln Vitro |
The dimeric structure provides high avidity binding to FAP with low nanomolar affinity. The chelator (DOTAGA) allows radiolabeling with diagnostic (e.g., ⁶⁸Ga, ¹⁸F) or therapeutic (e.g., ¹⁷⁷Lu, 22⁵Ac) radiometals without compromising FAP-binding affinity.
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| ln Vivo |
In tumor-bearing mice, ⁶⁸Ga-labeled DOTAGA-based FAPi dimers show high tumor uptake, rapid clearance from blood and non-target organs (primarily renal and hepatobiliary), and excellent tumor-to-background ratios on PET imaging, significantly outperforming monomeric FAP inhibitors.
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| Enzyme Assay |
The DOTAGA chelator is incubated with a radiometal (e.g., ⁶⁸GaCl3 in acetate buffer, pH 4.0) at 95degC for 10-15 min. Radiolabeling efficiency (>95%) is measured by radio-TLC or radio-HPLC. For FAP binding, the radiolabeled compound is incubated with FAP enzyme (0.1-10 nM), and inhibition is measured by fluorogenic substrate cleavage.
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| Cell Assay |
FAP-expressing cells (e.g., HT-1080-FAP, U87MG glioma) are incubated with radiolabeled or fluorescently labeled DOTAGA analogue (0.1-100 nM, 1 h at 37degC). Cell uptake is measured by gamma counting or flow cytometry. Specific binding is blocked with excess unlabeled FAPi to confirm target engagement.
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| Animal Protocol |
Mice bearing FAP-positive xenografts (e.g., HEK293-FAP, HT-1080-FAP) are injected intravenously with ⁶⁸Ga-labeled compound (e.g., 5-10 MBq, ~0.1-1 nmol). PET/CT imaging is performed at 1-4 h post-injection. Animals are then sacrificed; organs are excised, weighed, and counted in a gamma counter for biodistribution (%ID/g).
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| ADME/Pharmacokinetics |
⁶⁸Ga-labeled FAPi dimers show rapid blood clearance (t1/2 ~5-15 min), renal excretion as the primary pathway (urinary ~60-80% of injected dose by 1 h), and minimal hepatobiliary accumulation. Tumor uptake peaks at 1-2 h (typically 5-15%ID/g) and remains stable for several hours.
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| Toxicity/Toxicokinetics |
As a chelator-targeting ligand conjugate, the compound itself has no inherent toxicity. The final radiopharmaceutical's toxicity is primarily determined by the radionuclide. Preclinical studies show good tolerability at diagnostic imaging doses with no adverse effects on body weight or organ histology.
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| References | |
| Additional Infomation |
DOTAGA.(SA.FAPi)2 analogue is a research tool for molecular imaging. Similar FAPi-based radiotracers (e.g., ⁶⁸Ga-FAPI-46) have entered clinical trials for PET imaging of various cancers. This particular analogue is not FDA-approved; it is for preclinical research only.
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| Molecular Formula |
C75H89F7N18O19
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|---|---|
| Molecular Weight |
1679.61
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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 |
| 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 | 0.5954 mL | 2.9769 mL | 5.9538 mL | |
| 5 mM | 0.1191 mL | 0.5954 mL | 1.1908 mL | |
| 10 mM | 0.0595 mL | 0.2977 mL | 0.5954 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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