PRINOMASTAT HYDROCHLORIDE
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- CAS号:
- 1435779-45-5
- 英文名:
- Prinomastat hydrochloride
- 英文别名:
- KB-R9896 hydrochloride;(S)-N-Hydroxy-2,2-dimethyl-4-((4-(pyridin-4-yloxy)phenyl)sulfonyl)thiomorpholine-3-carboxamide hydrochloride
- 中文名:
- PRINOMASTAT HYDROCHLORIDE
- 中文别名:
- 化合物 T12539;(3S)-N-羟基-2,2-二甲基-4-[[4-(4-吡啶氧基)苯基]磺酰基]-3-硫代吗啉甲酰胺盐酸盐;(S)-N-羟基-2,2-二甲基-4-((4-(吡啶-4-基氧基)苯基)磺酰基)硫代吗啉-3-甲酰胺盐酸盐
- CBNumber:
- CB75821458
- 分子式:
- C18H22ClN3O5S2
- 分子量:
- 459.96
- MOL File:
- 1435779-45-5.mol
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PRINOMASTAT HYDROCHLORIDE化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 100 mg/mL (217.41 mM)
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形态:
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Solid
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颜色:
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White to off-white
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PRINOMASTAT HYDROCHLORIDE性质、用途与生产工艺
Prinomastat hydrochloride (AG3340 hydrochloride) 是一种广谱,有效的口服活性金属蛋白酶 (MMP) 抑制剂,对于 MMP-1, MMP-3 和 MMP-9 的 IC50 分别为 79 nM,6.3 nM 和 5.0 nM。Prinomastat hydrochloride 抑制 MMP-2, MMP-3 和 MMP-9 的 Ki 分别为 0.05 nM,0.3 nM 和 0.26 nM。Prinomastat hydrochloride 可穿过血脑屏障。抗肿瘤活性。
MMP-9
5 nM (IC
50
)
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MMP-9
0.26 nM (Ki)
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MMP-2
0.05 nM (Ki)
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MMP-1
79 nM (IC
50
)
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MMP-13
6.3 nM (IC
50
)
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MMP-13
0.3 nM (Ki)
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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.
Western Blot Analysis
Cell Line:
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C57MG/Wnt1 cells
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Concentration:
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0.1 µg/mL, 1 µg/mL
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Incubation Time:
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4 days
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Result:
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A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells.
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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.
PRINOMASTAT HYDROCHLORIDE
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1435779-45-5, PRINOMASTAT HYDROCHLORIDE 相关搜索:
- (S)-N-羟基-2,2-二甲基-4-((4-(吡啶-4-基氧基)苯基)磺酰基)硫代吗啉-3-甲酰胺盐酸盐
- (3S)-N-羟基-2,2-二甲基-4-[[4-(4-吡啶氧基)苯基]磺酰基]-3-硫代吗啉甲酰胺盐酸盐
- 化合物 T12539
- 1435779-45-5
- (S)-N-Hydroxy-2,2-dimethyl-4-((4-(pyridin-4-yloxy)phenyl)sulfonyl)thiomorpholine-3-carboxamide hydrochloride
- KB-R9896 hydrochloride