| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Prostate-specific membrane antigen (PSMA / FOLH1). PSMA is a type II transmembrane glycoprotein that is significantly overexpressed on the surface of prostate cancer cells and in the neovasculature of many solid tumors. PSMA617-TCMC TFA binds to the extracellular domain of PSMA with high affinity, enabling targeted delivery of diagnostic or therapeutic payloads to PSMA-expressing tissues.
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| ln Vitro |
In vitro characterization of PSMA617-TCMC TFA involves binding affinity assays using PSMA-expressing cell lines such as LNCaP or 22Rv1. Competitive binding studies with radiolabeled PSMA-617 are performed to determine IC50 and Ki values. Cell uptake and internalization assays are conducted by incubating cells with the compound at 37°C for various time points, followed by measurement of cell-associated radioactivity. The compound demonstrates high affinity and rapid internalization, characteristic of PSMA-targeting ligands.
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| ln Vivo |
In vivo studies of PSMA617-TCMC TFA are performed in mouse models bearing PSMA-positive tumor xenografts. Biodistribution studies involve intravenous administration of the radiolabeled compound, followed by ex vivo counting of radioactivity in tissues and tumors at various time points. Tumor uptake is expressed as percentage of injected dose per gram of tissue (%ID/g). The compound shows specific tumor accumulation and clearance from non-target organs. Imaging studies using SPECT or PET can visualize tumor targeting in live animals.
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| Enzyme Assay |
Cell-free binding assays for PSMA-targeting ligands typically use purified recombinant human PSMA protein immobilized on a solid support. The test compound is incubated with a fixed concentration of a radiolabeled reference ligand (e.g., ⁶⁸Ga-PSMA-11) in competition binding format. After incubation at room temperature for 1-2 hours, unbound ligand is removed by washing, and bound radioactivity is measured. IC50 values are calculated from competition curves using nonlinear regression. Surface plasmon resonance (SPR) can also be used to measure real-time binding kinetics (ka, kd, KD).
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| Cell Assay |
In vitro cellular assays use PSMA-positive cell lines such as LNCaP (human prostate adenocarcinoma) cultured in RPMI-1640 medium with 10% FBS. Cells are seeded in 24-well plates and allowed to attach overnight. Various concentrations of PSMA617-TCMC TFA (0.1-1000 nM) are added with a radiolabeled tracer, and cells are incubated at 4°C (for binding) or 37°C (for internalization) for 1-4 hours. Cell-associated radioactivity is measured after washing with cold PBS. Internalized fraction is determined by acid wash to remove surface-bound ligand. Saturation binding and competition assays are performed to calculate Bmax and Kd values.
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| Animal Protocol |
In vivo animal studies are conducted in immunodeficient mice (e.g., NSG or BALB/c nude) bearing subcutaneous PSMA-positive tumor xenografts. The radiolabeled compound is administered via tail vein injection at doses typically ranging from 0.1-1 nmol per animal. At predetermined time points (e.g., 1, 4, 24, 48 hours post-injection), animals are euthanized, and organs/tumors are collected, weighed, and counted in a gamma counter. Biodistribution data are expressed as %ID/g. Imaging studies using small-animal SPECT/CT or PET/CT are performed to visualize tumor targeting and whole-body distribution.
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| ADME/Pharmacokinetics |
As a PSMA-targeting ligand, PSMA617-TCMC TFA is expected to exhibit rapid blood clearance and predominant renal excretion, characteristic of small molecule PSMA ligands. When radiolabeled, the pharmacokinetics are determined by both the ligand properties and the radionuclide. The compound shows high tumor uptake and retention due to PSMA-mediated internalization, with favorable tumor-to-background ratios. Detailed PK parameters are typically determined in preclinical biodistribution studies using radiolabeled versions of the compound.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of PSMA617-TCMC TFA is typically performed in the context of its radiolabeled formulations. Non-radiolabeled PSMA ligands generally show low acute toxicity at preclinical doses. The TCMC modification may alter the chelation properties and thus the stability of the radiometal complex, which could impact toxicity profiles. Comprehensive toxicology data are generated as part of investigational new drug (IND) applications for PSMA-targeted radiopharmaceuticals. Standard safety pharmacology studies include assessments of cardiovascular, respiratory, and central nervous system function.
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| Additional Infomation |
PSMA617-TCMC TFA is a research compound designed for preclinical evaluation of PSMA-targeted theranostics. It is not an approved therapeutic agent. The compound is used to study structure-activity relationships of PSMA ligands and to optimize pharmacokinetic properties for improved tumor targeting. It is available from chemical suppliers for research purposes only. The TFA salt form enhances solubility and handling characteristics. Radiolabeling with various isotopes (⁶⁸Ga, ¹⁷⁷Lu, ²²⁵Ac) enables both diagnostic imaging and therapeutic applications in preclinical models.
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| Appearance |
Typically exists as solid 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.) |
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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