GCPII-IN-1
Based on 1 Customer Validation
GCPII-IN-1 (Compound 2) is a GCPII (also known as PSMA) inhibitor with a Ki of 44.3 nM. GCPII-IN-1 can be used in the research of prostate cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.83%
- CAS No.: 1025796-32-0
- Formule: C12H21N3O7
- Masse moléculaire:319.31
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-Prostate Cancer Compound Library
HY-L124
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Protease Inhibitor Library
HY-L147
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Amino Acid Metabolism Compound Library
HY-L189
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High-Throughput Bioactive Compound Library
HY-L205
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | CC50 |
>100 μM
Compound: DCL
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Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
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[PMID: 33822606] |
| HEK-293T | CC50 |
>100 μM
Compound: DCL
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Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 5 days by MTT assay
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[PMID: 33822606] |
| LNCaP | IC50 |
1470 nM
Compound: DCL
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Inhibition of PSMA in human LNCAP cells using NAAG as substrate measured after 2 hrs by amplex red reagent based fluorescence assay
Inhibition of PSMA in human LNCAP cells using NAAG as substrate measured after 2 hrs by amplex red reagent based fluorescence assay
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[PMID: 31248772] |
| LNCaP | IC50 |
498 nM
Compound: 10
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Inhibition of [131I]DCIT from PSMA in human LNCAP cells
Inhibition of [131I]DCIT from PSMA in human LNCAP cells
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[PMID: 19111054] |
| MCF7 | CC50 |
>100 μM
Compound: DCL
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Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
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[PMID: 33822606] |
| WI-38 VA13 | CC50 |
>100 μM
Compound: DCL
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Cytotoxicity against human VA13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human VA13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 31248772] |
| WI-38 VA13 | CC50 |
>100 μM
Compound: DCL
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Cytotoxicity against human WI-38 VA13 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Cytotoxicity against human WI-38 VA13 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
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[PMID: 33822606] |
GCPII-IN-1 (compound KUE) serves as a PSMA targeting vector to be conjugated with the zwitterionic metal chelators to generate probes for prostate cancer imaging applications[2].
GCPII-IN-1 can be radiolabeled with F-18 to be a PET agent for prostate cancer imaging[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1025796-32-0
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Appearance Solid
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Masse moléculaire 319.31
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Formule C12H21N3O7
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Color White to off-white
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SMILES
NCCCC[C@@H](C(O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (156.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Jan Tykvart, et al. Rational design of urea-based glutamate carboxypeptidase II (GCPII) inhibitors as versatile tools for specific drug targeting and delivery. Bioorg Med Chem. 2014 Aug 1;22(15):4099-108. [Content Brief]
[2]. John V. Frangioni, et al. Zwitterionic metal chelators. US20250082792A1. 2025-10-14.
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1318 mL | 15.6588 mL | 31.3175 mL | 78.2938 mL |
| 5 mM | 0.6264 mL | 3.1318 mL | 6.2635 mL | 15.6588 mL | |
| 10 mM | 0.3132 mL | 1.5659 mL | 3.1318 mL | 7.8294 mL | |
| 15 mM | 0.2088 mL | 1.0439 mL | 2.0878 mL | 5.2196 mL | |
| 20 mM | 0.1566 mL | 0.7829 mL | 1.5659 mL | 3.9147 mL | |
| 25 mM | 0.1253 mL | 0.6264 mL | 1.2527 mL | 3.1318 mL | |
| 30 mM | 0.1044 mL | 0.5220 mL | 1.0439 mL | 2.6098 mL | |
| 40 mM | 0.0783 mL | 0.3915 mL | 0.7829 mL | 1.9573 mL | |
| 50 mM | 0.0626 mL | 0.3132 mL | 0.6264 mL | 1.5659 mL | |
| 60 mM | 0.0522 mL | 0.2610 mL | 0.5220 mL | 1.3049 mL | |
| 80 mM | 0.0391 mL | 0.1957 mL | 0.3915 mL | 0.9787 mL | |
| 100 mM | 0.0313 mL | 0.1566 mL | 0.3132 mL | 0.7829 mL |
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