Prinomastat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Prinomastat (AG3340) 是一种有效的选择性 MMP 抑制剂，具有 pM 亲和力，可抑制明胶酶（MMP-2 和 -9，Ki=50-150 pM）。

Prinomastat (AG3340) is a potent, selective MMP inhibitor with pM affinities for inhibiting gelatinases (MMP-2 and -9, Ki=50-150 pM), MMP-14 and MMP-13; demonstrates broad antitumor activity in a number of tumor models, inhibits glioma invasion or growth of the human malignant glioma cell line U87; also suppresses tumor growth in a malignant glioma tumor model.Brain Cancer Phase 2 Discontinued.

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.

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.

AG3340

Metabolic Enzyme/Protease

MMP

MMP

Cancer

Brain Cancer

192329-42-3

423.502

C18H21N3O5S2

>98% (HPLC)

In Vitro:?DMSO : 2.5 mg/mL (5.90 mMul)

O=C([C@@H]1N(S(=O)(C2=CC=C(OC3=CC=NC=C3)C=C2)=O)CCSC1(C)C)NO

3-Thiomorpholinecarboxamide, N-hydroxy-2,2-dimethyl-4-[[4-(4-pyridinyloxy)phenyl]sulfonyl]-, (S)-

(-20℃)

With Ice Pack

≥ 2 years