| Description | Prinomastat (AG3340) is an orally active and selective inhibitor of metalloproteinases (MMPs) that crosses the blood-brain barrier. |
| In vitro | 在 C57MG/Wnt1 细胞中，Prinomastat（0.1 µg/mL，1 µg/mL；4天）能够显著降低 MMP-3 启动子活性[1]。 |
| In vivo | 在人类纤维肉瘤小鼠模型（HT1080）中，Prinomastat（50 mg/kg；腹腔注射）在动物体内耐受性良好，并表现出显著的肿瘤生长抑制作用。其半衰期为1.6小时。 |
| Target activity | MMP1:79 nM, MMP9:5 nM, MMP3:6..3 nM, MMP3:0.3 nM (ki), MMP2:0.05 nM (ki), MMP9:0.26 nM (ki) |
| Synonyms | KB-R9896, AG3340 |
| molecular weight | 423.51 |
| Molecular formula | C18H21N3O5S2 |
| CAS | 192329-42-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 1 mg/mL (2.36 mM), Sonication is recommended. H2O: 1 mg/mL (2.36 mM), Sonication and adjust pH to 3 with 1M HCl |
| References | 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. |