Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC 50 s of 79, 6.3 and 5.0 nM for MMP-1 , MMP-3 and MMP-9 , respectively. Prinomastat hydrochloride inhibits MMP-2 , MMP-3 and MMP-9 with K i s of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity. 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. 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). 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
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Prinomastat hydrochloride
CAS number：1435779-45-5 molecular formula：C18H22ClN3O5S2
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| Chinese alias | 盐酸普啉司他 | ||
| English alias | Q27273753 | N-hydroxy-2,2-dimethyl-4-[[4-(4-pyridinyloxy)phenyl]sulfonyl]-3-thiomorpholinecarboxamide, monohydrochloride | prinomastat HCl | (3S)-N-hydroxy-2,2-dimethyl-4-(4-pyridin-4-yloxyphenyl)sulfonylthiomorpholine-3-carboxamide;hydrochloride | F70895 | ||
| CAS number | 1435779-45-5 | molecular formula | C18H22ClN3O5S2 |
| molecular weight | 459.97 g/mol | Exact mass | - |
| PSA | 143.000 Ų | logp | - |
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