| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Biotin-NH-PSMA-617 specifically targets prostate-specific membrane antigen (PSMA), a transmembrane protein that is highly and consistently overexpressed on the surface of prostate cancer cells, particularly in metastatic, castration-resistant disease. The PSMA-617 moiety provides high binding affinity (KD in the low nanomolar range). The attached biotin group serves as a "molecular handle" for high-affinity capture by streptavidin or avidin in subsequent steps.
|
|---|---|
| ln Vitro |
PSMA-617 is a ligand for PSMA. PSMA-617 had a markedly enhanced affinity for binding PSMA and demonstrated effective internalization into PCa cells. PSMA-617 is suitable for radioligand-based treatments and PET imaging since it can be tagged with 68Ga, 177Lu, 111In, and 90Y [1].
In vitro, Biotin-NH-PSMA-617, as a PSMA ligand, demonstrates significantly enhanced binding affinity to PSMA and efficient internalization into prostate cancer (PCa) cells. The compound has been shown to be effectively internalized into PSMA-positive cells, a key requirement for targeted drug delivery. The biotin moiety does not interfere with this binding or internalization, making it an ideal pretargeting agent. |
| ln Vivo |
In vivo, Biotin-NH-PSMA-617 has shown promise in pretargeted imaging and therapy studies. In animal models, the biotinylated ligand rapidly localizes to PSMA-expressing tumors. When a radiolabeled streptavidin conjugate is subsequently administered, it quickly clears from the bloodstream and binds to the biotin on the tumor surface, resulting in high tumor-to-background contrast ratios. This pretargeting approach minimizes radiation exposure to healthy tissues.
|
| Enzyme Assay |
Non-cellular binding affinity of Biotin-NH-PSMA-617 for PSMA can be measured using Surface Plasmon Resonance (SPR) or competitive radioligand binding assays. In an SPR assay, recombinant PSMA protein is immobilized on a sensor chip. Increasing concentrations of the compound are flowed over the chip, and the association and dissociation rates (ka and kd) are measured to calculate the KD (equilibrium dissociation constant).
|
| Cell Assay |
Cellular assays are performed using PSMA-expressing human prostate cancer cell lines, such as LNCaP or C4-2. Cells are incubated with various concentrations of Biotin-NH-PSMA-617 at 4degC (for binding) or 37degC (for internalization). Binding and uptake are then detected using a fluorescently labeled streptavidin probe. The signal is quantified by flow cytometry, or the cells are imaged under a fluorescence microscope to visualize internalization.
|
| Animal Protocol |
A typical in vivo animal protocol involves two steps. First, a xenograft mouse model is established using PSMA-positive LNCaP or 22Rv1 cells. Biotin-NH-PSMA-617 is administered intravenously and allowed to circulate for 4-6 hours. Second, a radiolabeled streptavidin conjugate is injected intravenously. After an additional 6-24 hours, tumor uptake and biodistribution are assessed by gamma counting or PET/SPECT imaging of harvested organs.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) studies of Biotin-NH-PSMA-617 are typically conducted as part of the pretargeting workflow. The compound shows rapid blood clearance and specific retention in PSMA-positive tumors. The PEG linker in the compound contributes to optimal pharmacokinetics by improving its water solubility, reducing aggregation, and prolonging circulation time, which enhances tumor uptake before the second step of streptavidin injection.
|
| Toxicity/Toxicokinetics |
Dedicated toxicological studies for Biotin-NH-PSMA-617 are not detailed in standard product literature. As a research-use compound, standard safety assessments for acute toxicity are not typically described. However, because it is a targeted ligand that internalizes into PSMA-expressing cells, potential off-target toxicities would be related to PSMA expression in non-cancerous tissues, such as the proximal tubules of the kidney.
|
| References |
|
| Additional Infomation |
Biotin-NH-PSMA-617 has a molecular formula of C65H97N13O19S and a molecular weight of 1396.62 g/mol. It can be labeled with various radionuclides, including 68Ga, 177Lu, 111In, and 90Y, allowing for application in PET imaging and radioligand-based therapy. The compound represents a biotinylated "pretargeting" strategy for prostate cancer research. The product is intended for research use only and is not for human therapy.
|
| Molecular Formula |
C65H97N13O19S
|
|---|---|
| Molecular Weight |
1396.61
|
| Appearance |
White to off-white solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO :≥ 50 mg/mL (~35.80 mM)
|
|---|---|
| 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 | 0.7160 mL | 3.5801 mL | 7.1602 mL | |
| 5 mM | 0.1432 mL | 0.7160 mL | 1.4320 mL | |
| 10 mM | 0.0716 mL | 0.3580 mL | 0.7160 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
