Carboxypeptidase G2 (CPG2) InhibitorCPG2 Inhibitor CAS# 192203-60-4 |
- GAP-134
Catalog No.:BCC1588
CAS No.:943134-39-2
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 192203-60-4 | SDF | Download SDF |
| PubChem ID | 9796834 | Appearance | Powder |
| Formula | C13H15NO6S | M.Wt | 313.33 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | CPG2 Inhibitor | ||
| Solubility | H2O : 1.43 mg/mL (4.56 mM; Need ultrasonic) | ||
| Chemical Name | (2S)-2-[(4-methoxyphenyl)sulfanylcarbonylamino]pentanedioic acid | ||
| SMILES | COC1=CC=C(C=C1)SC(=O)NC(CCC(=O)O)C(=O)O | ||
| Standard InChIKey | OBCGYIKABKFIQB-JTQLQIEISA-N | ||
| Standard InChI | InChI=1S/C13H15NO6S/c1-20-8-2-4-9(5-3-8)21-13(19)14-10(12(17)18)6-7-11(15)16/h2-5,10H,6-7H2,1H3,(H,14,19)(H,15,16)(H,17,18)/t10-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents. References: | |||||
Carboxypeptidase G2 (CPG2) Inhibitor Dilution Calculator
Carboxypeptidase G2 (CPG2) Inhibitor Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1915 mL | 15.9576 mL | 31.9152 mL | 63.8305 mL | 79.7881 mL |
| 5 mM | 0.6383 mL | 3.1915 mL | 6.383 mL | 12.7661 mL | 15.9576 mL |
| 10 mM | 0.3192 mL | 1.5958 mL | 3.1915 mL | 6.383 mL | 7.9788 mL |
| 50 mM | 0.0638 mL | 0.3192 mL | 0.6383 mL | 1.2766 mL | 1.5958 mL |
| 100 mM | 0.0319 mL | 0.1596 mL | 0.3192 mL | 0.6383 mL | 0.7979 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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A novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
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Novel inhibitors of carboxypeptidase G2 (CPG2): potential use in antibody-directed enzyme prodrug therapy.[Pubmed:10090777]
J Med Chem. 1999 Mar 25;42(6):951-6.
The design and synthesis of potent thiocarbamate inhibitors for carboxypeptidase G2 are described. The best thiocarbamate inhibitor N-(p-methoxybenzenethiocarbonyl)amino-L-glutamic acid 6d, chosen for preliminary investigations of in vitro antibody-directed enzyme prodrug therapy (ADEPT), abrogated the cytotoxicity of a combination of A5B7-carboxypeptidase G2 conjugate and prodrug PGP (N-p-{N,N-bis (2-chloroethyl)amino}phenoxycarbonyl-L-glutamate) toward LS174T cells. This is the first report of a small-molecule enzyme inhibitor proposed for use in conjunction with the ADEPT approach.
Galactosylated antibodies and antibody-enzyme conjugates in antibody-directed enzyme prodrug therapy.[Pubmed:8306255]
Cancer. 1994 Feb 1;73(3 Suppl):1114-20.
Antibody directed enzyme prodrug therapy (ADEPT) has been studied as a two- and three-phase system in which an antibody to a tumor-associated antigen has been used to deliver an enzyme to tumor sites where it can convert a relatively nontoxic prodrug to a cytotoxic agent. In such a system, it is necessary to allow the enzyme activity to clear from the blood before prodrug injection to avoid toxicity caused by prodrug activation in plasma. To accelerate plasma clearance of enzyme activity, two approaches have been studied. The studies have been performed with a monoclonal anticarcinoembryonic-antigen antibody fragment A5B7-F(ab')2 conjugated to a bacterial enzyme, carboxypeptidase G2 (CPG2), in LS174T xenografted mice. In the first approach, a monoclonal antibody (SB43), directed at CPG2, was used, which inactivates CPG2 in vitro and in vivo. SB43 was galactosylated so that it had sufficient time to form a complex with plasma CPG2, resulting in the inactivation and clearance of the complex from plasma via the carbohydrate-specific receptors in the liver. Injection of SB43gal 19 hours after administration of the radiolabeled conjugate reduced the percentage of injected dose per gram in blood without affecting levels in the tumor. The second approach involved galactosylation of the conjugate so that it cleared rapidly from blood via the asialoglycoprotein receptors in the liver. Localization of the radiolabeled conjugate was achieved by blocking this receptor for about 8 hours with a single injection (8 mg/mouse) of an inhibitor that binds competitively to the receptor. This allowed tumor localization of the conjugate followed by a rapid clearance of the galactosylated conjugate from blood as the inhibitor was consumed. A tumor-to-blood ratio of 45:1 was obtained at 24 hours, which increased to 100:1 at 72 hours after the conjugate injection. These accelerated clearance mechanisms have been applied in antitumor studies in ADEPT.
