Prinomastat(Synonyms: 普啉司他; AG3340; KB-R9896)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Prinomastat (Synonyms: 普啉司他; AG3340; KB-R9896)

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-3 和 MMP-9 的 IC50 分别为 79 nM，6.3 nM 和 5.0 nM。Prinomastat 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 穿过血脑屏障。抗肿瘤活性。

Prinomastat(Synonyms: 普啉司他; AG3340; KB-R9896)

Prinomastat Chemical Structure

CAS No. : 192329-42-3

规格 价格 是否有货
1 mg ￥1250 询问价格 & 货期
5 mg ￥3750 询问价格 & 货期
10 mg ￥6550 询问价格 & 货期

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生物活性

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[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].

上海金畔生物科技有限公司 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.

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 T1/2 of 1.6 hours[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

423.51

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°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [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.

    [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.

    [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.

    [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.

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