| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
GCPII-IN-1 targets glutamate carboxypeptidase II (GCPII), also known as prostate-specific membrane antigen (PSMA). GCPII is a membrane-bound enzyme that is highly expressed in prostate cancer cells. GCPII-IN-1 binds the active site of GCPII with high affinity (Ki = 44.3 nM) and inhibits its enzymatic activity. It is used as a targeting vector for prostate cancer imaging.
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|---|---|
| ln Vitro |
In vitro, GCPII-IN-1 binds GCPII with a Ki of 44.3 nM. It is a low-molecular-weight, urea-based inhibitor scaffold. It specifically targets GCPII/PSMA. It is used as a research tool for prostate cancer imaging.
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| ln Vivo |
No independent in vivo efficacy data are widely reported for GCPII-IN-1. As a research compound, it is primarily used for in vitro and cellular studies. In vivo characterization, including pharmacokinetics, efficacy, and toxicity, has not been extensively reported. It is used as a targeting vector for imaging.
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| Enzyme Assay |
For non-cell enzyme assays, recombinant GCPII is incubated with GCPII-IN-1 and a radiolabeled or fluorescent substrate. Enzyme activity is measured by scintillation counting or fluorescence. Ki values are calculated from dose-response curves.
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| Cell Assay |
In cell assays, PSMA-positive prostate cancer cell lines (e.g., LNCaP) are treated with GCPII-IN-1. Cellular uptake is measured by fluorescence microscopy or flow cytometry. Cell viability is measured by MTT.
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| Animal Protocol |
No established in vivo animal protocol exists for GCPII-IN-1. If in vivo studies were conducted, the compound would be radiolabeled and administered intravenously in mice bearing PSMA-positive tumor xenografts. Tumor uptake would be measured by PET or SPECT imaging.
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| References |
| Molecular Formula |
C12H21N3O7
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|---|---|
| Molecular Weight |
319.3110435009
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| Exact Mass |
319.137
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| CAS # |
1025796-32-0
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| Related CAS # |
GCPII-IN-1 TFA;1269794-89-9
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| PubChem CID |
24952014
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| Appearance |
White to off-white solid powder
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| LogP |
-3.7
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
22
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| Complexity |
414
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(CCN)C[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O
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| InChi Key |
ZZASEPMMGWJWOV-YUMQZZPRSA-N
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| InChi Code |
InChI=1S/C12H21N3O7/c13-6-2-1-3-7(10(18)19)14-12(22)15-8(11(20)21)4-5-9(16)17/h7-8H,1-6,13H2,(H,16,17)(H,18,19)(H,20,21)(H2,14,15,22)/t7-,8-/m0/s1
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| Chemical Name |
(2S)-2-[[(1S)-5-amino-1-carboxypentyl]carbamoylamino]pentanedioic acid
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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) |
DMSO: ~50 mg/mL (~156.6 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (7.83 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1318 mL | 15.6588 mL | 31.3175 mL | |
| 5 mM | 0.6264 mL | 3.1318 mL | 6.2635 mL | |
| 10 mM | 0.3132 mL | 1.5659 mL | 3.1318 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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