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Purity: =99.29%
| Targets |
PSMA-11's primary target is prostate-specific membrane antigen (PSMA), a type II transmembrane protein that is overexpressed on the surface of prostate cancer cells. The compound is a ligand that binds to the extracellular structural domain of PSMA with high affinity. Upon intravenous administration of gallium Ga-68-labeled PSMA-11, the Glu-urea-Lys(Ahx) moiety targets and binds to PSMA-expressing tumor cells. Upon internalization, PSMA-expressing tumor cells can be detected during PET imaging.
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| ln Vitro |
In vitro, PSMA-11 binds to the extracellular structural domain of PSMA with high affinity and specificity. It is a ligand that targets PSMA-expressing cells. When labeled with a radiometal (e.g., gallium-68), it can be used to detect PSMA-expressing tumor cells in vitro using autoradiography or gamma counting. The compound's binding affinity and specificity make it a valuable tool for studying PSMA expression in prostate cancer.
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| ln Vivo |
In vivo, PSMA-11 is used as a PET tracer for the detection of prostate cancer recurrence and metastasis. When labeled with gallium Ga-68, it is administered intravenously to patients. The tracer accumulates in PSMA-expressing tumor cells, which can be visualized using PET imaging. PSMA-11 is also being studied for its potential to prevent or reduce salivary gland toxicity caused by PSMA-targeted radionuclides.
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| Enzyme Assay |
The in vitro activity of PSMA-11 is assessed using PSMA binding assays. PSMA-expressing cells (e.g., LNCaP prostate cancer cells) are incubated with radiolabeled PSMA-11 (e.g., ⁶⁸Ga-PSMA-11) in the presence of varying concentrations of unlabeled PSMA-11. The binding affinity (Kd) and specificity are determined by measuring the bound radioactivity. Competition binding assays can be performed using PSMA inhibitors to confirm specificity. For cell uptake studies, PSMA-expressing cells are incubated with radiolabeled PSMA-11, and the cellular uptake is measured over time.
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| Cell Assay |
For cellular assays, PSMA-expressing cell lines (e.g., LNCaP, PC3-PIP) and PSMA-negative cell lines (e.g., PC3) are used as controls. Cells are cultured in appropriate media and incubated with various concentrations of PSMA-11 (typically 0.1-100 nM) for defined periods. Cell-associated radioactivity is measured using a gamma counter. Internalization studies can be performed by stripping surface-bound radioactivity using an acidic buffer. Cell viability is assessed using standard assays to ensure that the compound does not affect cell viability at the concentrations used.
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| Animal Protocol |
In vivo, PSMA-11 is administered intravenously to patients or animal models. For PET imaging, patients are injected with ⁶⁸Ga-PSMA-11 (typically 100-200 MBq), and PET/CT or PET/MRI scans are performed 60-90 minutes after injection. The images are analyzed to detect PSMA-positive lesions. In preclinical studies, mice bearing PSMA-positive tumor xenografts are injected with radiolabeled PSMA-11, and biodistribution studies are performed by dissecting organs and measuring radioactivity.
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| ADME/Pharmacokinetics |
PSMA-11 has a molecular weight of 947.0 g/mol (net peptide). It is a small molecule ligand composed of a PSMA-targeting Glu-urea-Lys(Ahx) moiety linked to the HBED-CC chelator. The compound is soluble in water and DMSO. It should be stored at -20°C under appropriate conditions to maintain stability. For radiolabeling with gallium-68, the compound is typically dissolved in a suitable buffer and heated.
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| Toxicity/Toxicokinetics |
Specific toxicity data for PSMA-11 is not available in the provided search results. As a diagnostic agent, it is administered at very low doses (microgram quantities) and is not expected to cause significant toxicity. The primary safety concern is related to the radiation exposure from the gallium-68 label, which is minimized by using the lowest effective dose. The compound should be handled with appropriate radiation safety precautions when radiolabeled.
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| References |
: Meißner S, Janssen JC, Prasad V, Brenner W, Diederichs G, Hamm B, Hofheinz F, Makowski MR. Potential of asphericity as a novel diagnostic parameter in the evaluation of patients with (68)Ga-PSMA-HBED-CC PET-positive prostate cancer lesions. EJNMMI Res. 2017 Oct 23;7(1):85. doi: 10.1186/s13550-017-0333-9. PubMed PMID: 29058157; PubMed Central PMCID: PMC5651532.
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| Additional Infomation |
Gorzetide is an unlabeled radiotracer composed of a human prostate-specific membrane antigen (PSMA) targeting ligand linked to an acyclic radiometal chelator, N,N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid (HBED-CC), and may be used to prevent or reduce salivary gland toxicity caused by PSMA-targeted radionuclides. Injection of Gorzetide into the salivary glands selectively reduces the uptake of systemically administered PSMA-targeted radionuclides in saliva. This may reduce salivary gland toxicity caused by these drugs, including salivary gland hypofunction and xerostomia.
Drug Indications This drug is for diagnostic use only. Locametz, after being radiolabeled with gallium-68, is indicated for the detection of prostate-specific membrane antigen (PSMA)-positive lesions in adult patients with prostate cancer (PCa) via positron emission tomography (PET) in the following clinical settings: initial staging of high-risk PCa patients before radical treatment; screening for suspected PCa recurrence in patients with elevated serum PSA levels after radical treatment; and identification of patients with PSMA-positive progressive metastatic castration-resistant prostate cancer (mCRPC) who require PSMA-targeted therapy (see Section 4.4). PSMA-11 (Gozetotide) is a PSMA-targeting ligand used for PET imaging of prostate cancer. It is part of the ⁶⁸Ga-PSMA-11 PET tracer, which has been approved by the FDA for the detection of prostate cancer recurrence and metastasis. The tracer has been shown to have high sensitivity and specificity for PSMA-positive lesions, making it a valuable tool for prostate cancer staging and restaging. PSMA-11 is also being investigated for therapeutic applications, including targeted radionuclide therapy and prevention of salivary gland toxicity. It is available from chemical suppliers for research and clinical use. |
| Molecular Formula |
C44H62N6O17
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|---|---|
| Molecular Weight |
947.005
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| Exact Mass |
946.417
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| Elemental Analysis |
C, 55.81; H, 6.60; N, 8.87; O, 28.72
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| CAS # |
1366302-52-4
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| Related CAS # |
2412149-32-5 (TFA);1366302-52-4;PSMA-11 HCl;
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| PubChem CID |
60143283
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
1275.1±65.0 °C at 760 mmHg
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| Flash Point |
725.0±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.602
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| LogP |
0.2
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
35
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| Heavy Atom Count |
67
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| Complexity |
1620
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| Defined Atom Stereocenter Count |
2
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| SMILES |
OC1C=CC(CCC(NCCCCCC(NCCCC[C@@H](C(=O)O)NC(N[C@H](C(=O)O)CCC(=O)O)=O)=O)=O)=CC=1CN(CC(=O)O)CCN(CC(=O)O)CC1C(=CC=C(CCC(=O)O)C=1)O
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| InChi Key |
QJUIUFGOTBRHKP-LQJZCPKCSA-N
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| InChi Code |
InChI=1S/C44H62N6O17/c51-34-13-8-28(22-30(34)24-49(26-40(59)60)20-21-50(27-41(61)62)25-31-23-29(9-14-35(31)52)11-16-38(55)56)10-15-37(54)46-18-4-1-2-7-36(53)45-19-5-3-6-32(42(63)64)47-44(67)48-33(43(65)66)12-17-39(57)58/h8-9,13-14,22-23,32-33,51-52H,1-7,10-12,15-21,24-27H2,(H,45,53)(H,46,54)(H,55,56)(H,57,58)(H,59,60)(H,61,62)(H,63,64)(H,65,66)(H2,47,48,67)/t32-,33-/m0/s1
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| Chemical Name |
(3S,7S)-22-(3-(((2-((5-(2-Carboxyethyl)-2-hydroxybenzyl)(carboxymethyl)amino)ethyl)(carboxymethyl)amino)methyl)-4-hydroxyphenyl)-5,13,20-trioxo-4,6,12,19-tetraazadocosane-1,3,7-tricarboxylic acid
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| Synonyms |
Psma-hbed-CC PSMA-11 PSMA11 PSMA 11 HBED-CC-PSMA.
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~105.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.64 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 (2.64 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 (2.64 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 | 1.0560 mL | 5.2798 mL | 10.5596 mL | |
| 5 mM | 0.2112 mL | 1.0560 mL | 2.1119 mL | |
| 10 mM | 0.1056 mL | 0.5280 mL | 1.0560 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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