Prinomastat
Based on 4 publication(s) in Google Scholar
Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3, MMP-13 and MMP-9 with Kis of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.41%
- CAS No.: 192329-42-3
- Formule: C18H21N3O5S2
- Masse moléculaire:423.51
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Publications Citing Use of MedChemExpress (MCE) Prinomastat
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Activité biologique
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MMP-9 5 nM (IC50) |
MMP-9 0.26 nM (Ki) |
MMP-2 0.05 nM (Ki) |
MMP-1 79 nM (IC50) |
MMP-3 6..3 nM (IC50) |
MMP-3 0.3 nM (Ki) |
collagenases 3 0.03 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>500 μM
Compound: Prinomastat
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31415980] |
| HL-60 | IC50 |
>500 μM
Compound: Prinomastat
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Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31415980] |
| HUVEC | IC50 |
>500 μM
Compound: Prinomastat
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Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31415980] |
| K562 | IC50 |
>500 μM
Compound: Prinomastat
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Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31415980] |
| KG-1 | IC50 |
>500 μM
Compound: Prinomastat
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Antiproliferative activity against human KG1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human KG1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31415980] |
| MCF7 | IC50 |
>500 μM
Compound: Prinomastat
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31415980] |
| PC-3 | IC50 |
>500 μM
Compound: Prinomastat
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Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31415980] |
| THP-1 | IC50 |
8600 nM
Compound: 2Prinomastat
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Selective inhibition of the cellular TNF alpha release from LPS-stimulated THP-1 cells
Selective inhibition of the cellular TNF alpha release from LPS-stimulated THP-1 cells
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[PMID: 11754593] |
Prinomastat (AG3340; 0.1-1 μg/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat[1].
Co-culture of L/Wnt3a cells and CT7 cells increases the Topflash activity in CT7 cells, and co-culturing both L/Wnt3a cells and MMP-3 overexpressing C57MG cells with CT7 cells increases the Topflash luciferase activity in CT7 cells beyond the level observed with L/Wnt3a cells, and these effects are all suppressed by Prinomastat (AG3340)[1].
Inhibition of entry of C57MG/Wnt1 cells into S phase by Prinomastat corresponds to a decrease in expression of cyclin D1 and Erk1/2 phosphorylation. The effect of Prinomastat on Wnt1-induced migration is then examined using an in vitro wound assay. As anticipated, the migration of C57MG/Wnt1 cells is increased by 1.8-fold when compared with C57MG cells.The effect of Wnt1 on the cellular distribution of vimentin is reversed by Prinomastat in C57MG/Wnt1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C57MG/Wnt1 cells
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Concentration:0.1 µg/mL, 1 µg/mL
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Incubation Time:4 days
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Result:A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 192329-42-3
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Appearance Solid
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Masse moléculaire 423.51
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Formule C18H21N3O5S2
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Color White to off-white
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SMILES
O=C([C@@H]1N(S(=O)(C2=CC=C(OC3=CC=NC=C3)C=C2)=O)CCSC1(C)C)NO
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Synonyms
AG3340; KB-R9896
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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
Publications (4)
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Journal Impact Factor
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Most Recent
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Sci Adv
2023 Jan 20;9(3):eadd3867. PMID: 36662861 -
J Neuropathol Exp Neurol
Inhibiting Matrix Metalloproteinases Protects Evoked Electromyography Amplitudes and Muscle Tension in the Orbicularis Oris Muscle in a Rat Model of Facial Nerve Injury. [Abstract]2022 Sep 19;81(10):816-824. PMID: 35656867 -
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Solvant et solubilité
1 M HCl : 25 mg/mL (59.03 mM; Need ultrasonic)
H2O : 2.5 mg/mL (5.90 mM; ultrasonic and adjust pH to 3 with HCl)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (280 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Sørensen MD, et al. Cyclic phosphinamides and phosphonamides, novel series of potent matrix metalloproteinase inhibitors with antitumour activity. Bioorg Med Chem. 2003 Dec 1;11(24):5461-84. [Content Brief]
[2]. Blavier L, et al. Stromelysin-1 (MMP-3) is a target and a regulator of Wnt1-induced epithelial-mesenchymal transition (EMT). Cancer Biol Ther. 2010 Jul 15;10(2):198-208. [Content Brief]
[3]. Shalinsky DR, et al. Broad antitumor and antiangiogenic activities of AG3340, a potent and selective MMP inhibitor undergoing advanced oncology clinical trials. Ann N Y Acad Sci. 1999 Jun 30;878:236-70. [Content Brief]
[4]. Ozerdem U, et al. The effect of prinomastat (AG3340), a potent inhibitor of matrix metalloproteinases, on a subacute model of proliferative vitreoretinopathy. Curr Eye Res. 2000 Jun;20(6):447-53. [Content Brief]
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 |
|---|---|---|---|---|---|
| H2O / 1 M HCl | 1 mM | 2.3612 mL | 11.8061 mL | 23.6122 mL | 59.0305 mL |
| 5 mM | 0.4722 mL | 2.3612 mL | 4.7224 mL | 11.8061 mL | |
| 1 M HCl | 10 mM | 0.2361 mL | 1.1806 mL | 2.3612 mL | 5.9030 mL |
| 15 mM | 0.1574 mL | 0.7871 mL | 1.5741 mL | 3.9354 mL | |
| 20 mM | 0.1181 mL | 0.5903 mL | 1.1806 mL | 2.9515 mL | |
| 25 mM | 0.0944 mL | 0.4722 mL | 0.9445 mL | 2.3612 mL | |
| 30 mM | 0.0787 mL | 0.3935 mL | 0.7871 mL | 1.9677 mL | |
| 40 mM | 0.0590 mL | 0.2952 mL | 0.5903 mL | 1.4758 mL | |
| 50 mM | 0.0472 mL | 0.2361 mL | 0.4722 mL | 1.1806 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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