普马司他

生物活性靶点体外研究体内研究普马司他试剂级价格

普马司他

CAS号:192329-42-3
英文名:Prinomastat
中文名:普马司他
CBNumber:CB01475597
分子式:C18H21N3O5S2
分子量:423.51
MOL File:192329-42-3.mol

普马司他化学性质

熔点 :149.8°
密度 :1.377±0.06 g/cm3(Predicted)
储存条件 :room temp
溶解度 :H2O: soluble15mg/mL (clear solution)
形态 :powder
酸度系数(pKa) :9.25±0.23(Predicted)
颜色 :white to beige

安全信息

危险品标志 :T
危险类别码 :60-61
安全说明 :53-45
WGK Germany :3

普马司他性质、用途与生产工艺

生物活性 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。

靶点

MMP-9

5 nM (IC ₅₀ )

MMP-9

0.26 nM (Ki)

MMP-2

0.05 nM (Ki)

MMP-1

79 nM (IC ₅₀ )

MMP-3

6..3 nM (IC ₅₀ )

MMP-3

0.3 nM (Ki)

体外研究

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:	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 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.