| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PSMA I&S TFA targets the prostate-specific membrane antigen (PSMA), a type II transmembrane protein that is highly expressed on the surface of prostate cancer cells. PSMA expression is upregulated in aggressive and metastatic prostate cancer, making it a clinically validated target for imaging and therapy. The compound consists of a PSMA-binding motif and a chelator moiety that can be radiolabeled with technetium-99m (⁹⁹ᵐTc).
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| ln Vitro |
PSMA I&S TFA is a precursor of a 99mTc-labeled PSMA-targeting ligand. The compound itself is not biologically active until radiolabeled. Once labeled with ⁹⁹ᵐTc, the resulting radiopharmaceutical binds to PSMA with high affinity. The molecular structure features a technetium core complexed with the peptide, which enhances its binding affinity to target cells. It is designed for advanced ophthalmic and age-related macular degeneration (AMD) studies.
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| ln Vivo |
In vivo, the ⁹⁹ᵐTc-labeled PSMA-targeting ligand derived from PSMA I&S TFA is used for SPECT imaging of PSMA-expressing tumors. The radiotracer localizes to PSMA-positive prostate cancer cells, allowing visualization of primary and metastatic lesions. The compound has garnered attention in prostate cancer diagnostics and therapy, with detailed research findings on its synthesis, binding affinity, biodistribution, and clinical applications.
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| Enzyme Assay |
A cell-free binding assay for PSMA I&S TFA is performed after radiolabeling. PSMA I&S TFA is radiolabeled with ⁹⁹ᵐTc following standard procedures. Radiolabeled compound (0.1-10 nM) is incubated with recombinant PSMA protein or PSMA-expressing cell membranes in binding buffer (50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 0.1% BSA). Nonspecific binding is determined in the presence of excess unlabeled PSMA inhibitor. Bound radioactivity is separated by filtration and counted using a gamma counter.
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| Cell Assay |
PSMA I&S TFA is a precursor and is not used directly in cell-based assays. Instead, the radiolabeled product is used. PSMA-positive cells (e.g., LNCaP prostate cancer cells) and PSMA-negative cells (e.g., PC3 cells) are seeded in 24-well plates. Radiolabeled PSMA-targeting ligand (1-100 nM) is added and incubated for 1-2 hours at 4degC or 37degC. Cells are washed, and cell-associated radioactivity is measured by gamma counter. Internalization is assessed by acid wash. Binding specificity is confirmed by competition with excess unlabeled ligand.
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| Animal Protocol |
A standard in vivo protocol involves a mouse xenograft model of prostate cancer. Male BALB/c nude mice are implanted subcutaneously with LNCaP cells (PSMA-positive) or PC3 cells (PSMA-negative). When tumors reach appropriate size, the radiolabeled PSMA-targeting ligand derived from PSMA I&S TFA is administered intravenously (100-200 uCi, 10-50 ug). Mice are imaged by SPECT at various time points (1, 4, 24 hours post-injection). Biodistribution is measured by dissecting organs and counting radioactivity.
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| ADME/Pharmacokinetics |
PSMA I&S TFA has a molecular weight of 1413.43 and the molecular formula C61H83F3N10O23S. It is a solid that can be stored at -20degC, protected from light and moisture. The TFA salt is the standard form for handling. For radiolabeling, the precursor is dissolved in DMSO or water. Specific PK parameters of the precursor have not been reported; the radiolabeled ligand is rapidly cleared from the bloodstream via renal excretion.
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| Toxicity/Toxicokinetics |
PSMA I&S TFA is a precursor for radiolabeling and is not intended for direct therapeutic administration. The unlabeled precursor is considered to have low inherent toxicity. The radiolabeled ligand involves exposure to radioactive technetium-99m, which carries radiation safety risks. Standard radiation safety protocols must be followed when handling and administering the radiolabeled product. No other toxicity data are available.
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| References | |
| Additional Infomation |
PSMA I&S TFA is a research-grade precursor for the development of ⁹⁹ᵐTc-labeled PSMA-targeting radiopharmaceuticals. It is used for imaging and potential therapy of prostate cancer. The product is for research use only and is not approved for clinical diagnostic or therapeutic applications. The TFA salt is the standard commercial form. This product is for research use only.
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| Molecular Formula |
C61H83F3N10O23S
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|---|---|
| Molecular Weight |
1413.43
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| Related CAS # |
PSMA I&S;2639475-07-1
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| Appearance |
White to off-white 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). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 :~100 mg/mL (~70.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7075 mL | 3.5375 mL | 7.0750 mL | |
| 5 mM | 0.1415 mL | 0.7075 mL | 1.4150 mL | |
| 10 mM | 0.0707 mL | 0.3537 mL | 0.7075 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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