| Description | Prinomastat hydrochloride is a orally active inhibitor of metalloproteinase (MMP)(MMP-1, MMP-3 and MMP-9 with IC50s of 79, 6.3 and 5.0 nM , respectively),with Antitumor avtivity. |
| In vitro | Prinomastat inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat[1]. |
| In vivo | Prinomastat has good tumour growth inhibition, with a short T1/2 of 1.6 hours[1]. |
| Target activity | MMP1:79 nM, MMP2:0.05 nM (ki), MMP13:0.3 nM (ki), MMP13:6.3 nM, MMP9:0.26 nM (ki), MMP9:5 nM |
| Synonyms | KB-R9896 hydrochloride, AG3340 hydrochloride |
| molecular weight | 459.97 |
| Molecular formula | C18H22ClN3O5S2 |
| CAS | 1435779-45-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (217.41 mM), Sonication is recommended. |
| 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. |