Art. -Nr.: HY-12170

Prinomastat

Name: Prinomastat
Brand: MedChemExpress
SKU: HY-12170
Price: 125.00 USD
Availability: InStock
Rating: 5 (4 reviews)

(Synonyms: AG3340; KB-R9896)

4 Cited Publications

Kundenbewertung

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 K_is of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 98.41%
CAS. Nr.: 192329-42-3
Formel: C₁₈H₂₁N₃O₅S₂
Molecular Weight:423.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Prinomastat Chemical Structure

CAS. Nr.: 192329-42-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]^[3]^[4]

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)

Alle MMP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>500 μM Compound: Prinomastat	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	[PMID: 31415980]
HL-60	IC₅₀	>500 μM Compound: Prinomastat	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	[PMID: 31415980]
HUVEC	IC₅₀	>500 μM Compound: Prinomastat	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	[PMID: 31415980]
K562	IC₅₀	>500 μM Compound: Prinomastat	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	[PMID: 31415980]
KG-1	IC₅₀	>500 μM Compound: Prinomastat	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	[PMID: 31415980]
MCF7	IC₅₀	>500 μM Compound: Prinomastat	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	[PMID: 31415980]
PC-3	IC₅₀	>500 μM Compound: Prinomastat	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	[PMID: 31415980]
THP-1	IC₅₀	8600 nM Compound: 2Prinomastat	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	[PMID: 11754593]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

C57MG/Wnt1 cells
Concentration:

0.1 µg/mL, 1 µg/mL
Incubation Time:

4 days
Result:

A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells.

In Vivo

In a human fibrosarcoma mouse model (HT1080), the mice are treated therapeutically for 14-16 days with 50 mg/kg/day ip daily starting day 3 to 6 after tumour inoculation. Prinomastat is well tolerated by the animals, and there are no signs of weight loss or other adverse effects. Prinomastat has good tumour growth inhibition, with a short T_1/2 of 1.6 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 192329-42-3
Appearance Solid
Molecular Weight 423.51
Formel C₁₈H₂₁N₃O₅S₂
Color White to off-white
SMILES

O=C([C@@H]1N(S(=O)(C2=CC=C(OC3=CC=NC=C3)C=C2)=O)CCSC1(C)C)NO
Synonyms

AG3340; KB-R9896
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

All

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Journal Impact Factor

Sci Adv

Altered host protease determinants for SARS-CoV-2 Omicron. [Abstract]

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
bioRxiv

2026 Jan 2.
KTH Royal Institute of Technology

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (236.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3612 mL

11.8061 mL

23.6122 mL

5 mM

0.4722 mL

2.3612 mL

4.7224 mL

10 mM

0.2361 mL

1.1806 mL

2.3612 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.90 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.90 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	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
	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
	60 mM	0.0394 mL	0.1968 mL	0.3935 mL	0.9838 mL
	80 mM	0.0295 mL	0.1476 mL	0.2952 mL	0.7379 mL
	100 mM	0.0236 mL	0.1181 mL	0.2361 mL	0.5903 mL

Bioz

Prinomastat

4 Cited Publications

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Prinomastat

Publications Citing Use of MedChemExpress (MCE) Prinomastat

Alle MMP Isoform-spezifische Produkte anzeigen