Comparison

Prinomastat

Item no. CS-7961-10mg
Manufacturer ChemScene
Amount 10mg
Category
Type Molecules
Specific against other
ECLASS 10.1 32169090
ECLASS 11.0 32169090
UNSPSC 12000000
Alias 192329-42-3
Similar products 192329-42-3
Available
Alternative Names
AG3340; KB-R9896
CAS
192329-42-3
Purity
>98%
MWt
423.51
Formula
C18H21N3O5S2
Solubility
10 mM in DMSO
Clinical Information
Phase 3
Pathway
Metabolic Enzyme/Protease
Target
MMP
Biological Activity
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 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity[1][2][3][4]. IC50 & Target: IC50: 79 nM (MMP-1), 6.3 nM (MMP-3), 5.0 nM (MMP-9)[1] In Vitro: Prinomastat (AG3340; 0.1-1 ug/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and beta-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]. 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 T1/2 of 1.6 hours[1].
Research Area
Cancer

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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 10mg
Available: In stock
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