| Size | Price | |
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| 5mg | ||
| 10mg | ||
| 50mg | ||
| 100mg | ||
| Other Sizes |
| Targets |
The target of [¹⁸F]PSMA-1007 is prostate-specific membrane antigen (Glutamate Carboxypeptidase 2, GCPII/PSMA). PSMA is a type II transmembrane glycoprotein with limited expression in normal prostate epithelial cells but is significantly overexpressed in prostate cancer cells, with expression levels rising with increasing tumor dedifferentiation and hormone resistance. Following intravenous injection, the PSMA-1007 ligand moiety of [¹⁸F]PSMA-1007 specifically binds to PSMA-positive tumor cells, and the positrons emitted by the radioisotope fluorine-18 enable non-invasive visualization of PSMA-expressing tumors via PET/CT or PET/MRI imaging.
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| ln Vitro |
In in vitro PSMA binding affinity assays, the PSMA-1007 ligand exhibits a binding affinity of 6.7 ± 1.7 nM for PSMA. In PSMA-positive LNCaP cells, PSMA-1007 demonstrates an exceptionally high internalization rate (67% ± 13%), indicating that the ligand not only binds efficiently to PSMA but is also internalized into cells, making its structure compatible with therapeutic PSMA-617 radioligands. This favorable internalization property is an important basis for its use as a companion diagnostic agent in theranostic approaches.
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| ln Vivo |
[¹⁸F]PSMA-1007 demonstrates excellent tumor-targeting performance in vivo. In LNCaP tumor-bearing nude mouse models, the peak tumor uptake concentration reaches 2.8%ID/g (112 minutes post-injection), with a tumor absorbed dose of 0.079 ± 0.010 Gy/MBq. In organ distribution studies in tumor-bearing mice, LNCaP tumors show a specific uptake value of 8.0 ± 2.4 %ID/g. Small-animal PET/CT experiments clearly visualize LNCaP tumors. In clinical studies, a study of 10 patients with high-risk prostate cancer reported that [¹⁸F]PSMA-1007 PET/CT detected 18 of 19 pelvic lymph node metastases, with the smallest detectable lymph node being only 1 mm in diameter. In a Japanese Phase I/IIa study, using both pathology and imaging as the gold standard, [¹⁸F]PSMA-1007 achieved 100% sensitivity and 100% positive predictive value.
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| Enzyme Assay |
The PSMA binding affinity of the PSMA-1007 ligand is determined using radioligand competitive binding assays. The experimental procedure is as follows: PSMA-positive LNCaP cell membrane homogenates or purified recombinant PSMA protein are incubated with fixed concentrations of radiolabeled reference ligands (such as ¹²⁵I-MIP-1072 or ³H-PSMA-617) and increasing concentrations of unlabeled PSMA-1007 (typically ranging from 0.01 nM to 100 μM) in binding buffer at room temperature for 1-2 hours. After incubation, bound and free fractions are separated by rapid filtration through glass fiber filters, and residual radioactivity on the filters is measured using a γ-counter or liquid scintillation counter. IC₅₀ values are calculated by nonlinear regression analysis, and Ki values are derived using the Cheng-Prusoff equation. PSMA-1007 exhibits a Ki value of 6.7 ± 1.7 nM.
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| Cell Assay |
Cellular characterization of PSMA-1007 is evaluated via internalization assays using PSMA-positive cell lines. A typical procedure is as follows: PSMA-positive LNCaP cells and PSMA-negative PC-3 cells (as negative control) are seeded in 24-well plates (1-2×10⁵ cells per well) and cultured in RPMI-1640 medium containing 10% FBS at 37°C, 5% CO₂ until adherent. Cells are incubated with radiolabeled [¹⁸F]PSMA-1007 (typically 0.1-1 μCi/well) at 37°C for various time points (e.g., 10, 30, 60, 120, 240 minutes). Following incubation, cells are washed with acidic buffer (0.05 M glycine-HCl, pH 2.8) to remove surface-bound ligand, then lysed with NaOH. Surface-bound and internalized radioactivities are measured separately using a γ-counter. The internalization rate is expressed as the percentage of internalized radioactivity relative to total bound radioactivity. PSMA-1007 exhibits an internalization rate of 67% ± 13%.
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| Animal Protocol |
Preclinical in vivo studies of [¹⁸F]PSMA-1007 are performed using subcutaneous LNCaP prostate cancer xenograft mouse models. The experimental procedure is as follows: 1.0 × 10⁷ LNCaP cells (suspended in 200 μL PBS) are inoculated into the right flank of 6-week-old male BALB/c nude mice, and PET/CT imaging is performed when tumor volumes reach approximately 0.5-0.7 cm³. [¹⁸F]PSMA-1007 is administered as a single injection via the tail vein at a dose of 3.7-11.1 MBq, and dynamic (0-120 minutes) and static scans are acquired using a dedicated small-animal PET/CT system. Regions of interest are drawn to determine radioactive uptake in various organs and tumors, expressed as %ID/g. Specific binding studies are performed using pretreatment with the PSMA inhibitor 2-PMPA (2-(phosphonomethyl)-pentanedioic acid), which reduces tumor uptake by 32%. Repeatability studies show a within-subject coefficient of variation of 7.57% for net influx rates.
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| ADME/Pharmacokinetics |
The pharmacokinetic profile of [¹⁸F]PSMA-1007 has been characterized in humans and animal models. In healthy volunteers, following a single intravenous injection of 3.7 MBq/kg [¹⁸F]PSMA-1007, the mean blood radioactivity concentration peaks at 5 minutes (47.87 ± 1.05 %ID/mL) and declines to 1.60 ± 0.78 %ID/mL at 6 hours; whole-body radioactivity peaks at 5 minutes (211.05 ± 6.77 × 10³ %ID) and declines to 7.18 ± 3.91 × 10³ %ID at 6 hours. The tracer is primarily excreted via the hepatobiliary pathway with negligible urinary clearance, resulting in low bladder radioactivity that facilitates evaluation of the primary prostate tumor and pelvic lymph nodes. The effective dose of the radiopharmaceutical is approximately 4.4-5.5 mSv per examination (200-250 MBq injection dose). In LNCaP tumor-bearing mouse models, the peak tumor uptake is observed at 112 minutes post-injection (2.8%ID/g).
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| Toxicity/Toxicokinetics |
As a diagnostic radiopharmaceutical, the toxicity of [¹⁸F]PSMA-1007 primarily involves two aspects: the chemical toxicity of the drug itself and radiation exposure risk. In Phase I/IIa clinical trials involving healthy volunteers and prostate cancer patients, all subjects tolerated [¹⁸F]PSMA-1007 well, and no serious adverse events or drug-related adverse reactions were observed. The summary report on marketing authorization also confirms that no undesirable effects associated with [¹⁸F]PSMA-1007 in clinical use have been reported to date. The drug contributes to patients' long-term cumulative radiation exposure, which is associated with an increased risk of cancer. Contraindications include hypersensitivity to the active substance or any of the excipients. Additionally, case reports indicate that [¹⁸F]PSMA-1007 may show false-positive uptake in benign ganglia and lipomas, highlighting the need for careful interpretation.
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| References | |
| Additional Infomation |
Fluorine-18 PSMA-1007 is a radioconjugate containing the human prostate-specific membrane antigen (PSMA) targeting ligand PSMA-1007 and labeled with the radioisotope fluorine-18, possessing potential imaging activity for positron emission tomography/computed tomography (PET/CT). After injection of fluorine-18 PSMA-1007, PSMA-1007 partially targets and binds to PSMA-expressing tumor cells. This allows for the observation of PSMA-expressing cells during imaging. PSMA is a tumor-associated antigen (TAA) and type II transmembrane protein expressed on the prostate epithelial cell membrane and is highly overexpressed in prostate cancer (PCa) cells, with expression levels increasing with tumor differentiation and in hormone-resistant cancers.
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| Molecular Formula |
C49H55FN8O16
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|---|---|
| Molecular Weight |
1030.00595116615
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| Exact Mass |
1030.37
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| Elemental Analysis |
C, 57.08; H, 5.38; F, 1.84; N, 10.87; O, 24.83
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| CAS # |
2093321-19-6
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| Related CAS # |
2226894-58-0
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| PubChem CID |
145996605
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| Appearance |
White to off-white solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
30
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| Heavy Atom Count |
74
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| Complexity |
1970
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC=C2C=C(C=CC2=C1)C[C@@H](C(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O)NC(=O)C3=CC=C(C=C3)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)C4=CN=C(C=C4)[18F]
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| InChi Key |
RFFFFGRYVZESLB-LTLCPEALSA-N
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| InChi Code |
InChI=1S/C49H55FN8O16/c50-38-18-14-32(26-52-38)43(66)54-34(16-20-40(61)62)46(69)55-33(15-19-39(59)60)44(67)53-25-27-8-12-30(13-9-27)42(65)56-37(24-28-10-11-29-5-1-2-6-31(29)23-28)45(68)51-22-4-3-7-35(47(70)71)57-49(74)58-36(48(72)73)17-21-41(63)64/h1-2,5-6,8-14,18,23,26,33-37H,3-4,7,15-17,19-22,24-25H2,(H,51,68)(H,53,67)(H,54,66)(H,55,69)(H,56,65)(H,59,60)(H,61,62)(H,63,64)(H,70,71)(H,72,73)(H2,57,58,74)/t33-,34-,35-,36-,37-/m0/s1
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| Chemical Name |
(((S)-1-carboxy-5-((S)-2-(4-(((S)-4-carboxy-2-((S)-4-carboxy-2-(6-fluoronicotinamido)butanamido)butanamido)methyl)benzamido)-3-(naphthalen-2-yl)propanamido)pentyl)carbamoyl)-L-glutamic acid
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| Synonyms |
PSMA-1007; PSMA1007; PSMA 1007;
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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 | 0.9709 mL | 4.8543 mL | 9.7086 mL | |
| 5 mM | 0.1942 mL | 0.9709 mL | 1.9417 mL | |
| 10 mM | 0.0971 mL | 0.4854 mL | 0.9709 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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