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Prinomastat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Prinomastat图片
CAS NO:192329-42-3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
普啉司他
AG3340
KB-R9896
产品介绍
Prinomastat (AG3340) 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-3MMP-9IC50分别为 79 nM,6.3 nM 和 5.0 nM。Prinomastat 抑制MMP-2,MMP-3MMP-9Ki分别为 0.05 nM,0.3 nM 和 0.26 nM。Prinomastat 穿过血脑屏障。抗肿瘤活性。
生物活性

Prinomastat (AG3340) is a broad spectrum, potent, orally activemetalloproteinase (MMP)inhibitor withIC50s of 79, 6.3 and 5.0 nM forMMP-1,MMP-3andMMP-9, respectively. Prinomastat inhibitsMMP-2,MMP-3andMMP-9withKis 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[1][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)

体外研究
(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].

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.
体内研究
(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 T1/2of 1.6 hours[1].

Clinical Trial
分子量

423.51

性状

Solid

Formula

C18H21N3O5S2

CAS 号

192329-42-3

中文名称

普啉司他

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO :< 1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble or slightly soluble)