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Prinomastat hydrochloride
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 hydrochloride图片
CAS NO:1435779-45-5
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议

产品名称
AG3340 hydrochloride
KB-R9896 hydrochloride
产品介绍
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。
生物活性

Prinomastat hydrochloride (AG3340 hydrochloride) 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 hydrochloride inhibitsMMP-2,MMP-3andMMP-9withKis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross 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-13

6.3 nM (IC50)

MMP-13

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

459.97

性状

Solid

Formula

C18H22ClN3O5S2

CAS 号

1435779-45-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(217.41 mM;Need ultrasonic)

H2O : 50 mg/mL(108.70 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1741 mL10.8703 mL21.7405 mL
5 mM0.4348 mL2.1741 mL4.3481 mL
10 mM0.2174 mL1.0870 mL2.1741 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。