| 产品描述： | Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes |
| 靶点： |
MMP-3:3 nM (IC50);MMP-1:5 nM (IC50);MMP-2:6 nM (IC50);MMP-14:9 nM (IC50);MMP-7:13 nM (IC50);MMP |
| 体内研究： |
Animals receiving chemoradiation + Marimastat (BB2516) (8.7 mg/kg) have statistically significant delayed growth, compared to animals receiving chemoradiation alone. Marimastat (BB2516) may work in combination with chemotherapy and radiation to inhibit tumor growth |
| 参考文献： |
1. Rasmussen HS, et al. Matrix metalloproteinase inhibition as a novel anticancer strategy: a review with special focus on batimastat and marimastat. Pharmacol Ther. 1997;75(1):69-75. 2. Yu M, et al. Incorporation of Bulky and Cationic Cyclam-Triazole Moieties into Marimastat Can Generate Potent MMP Inhibitory Activity without Inducing Cytotoxicity. ChemistryOpen. 2013 Jun;2(3):99-105. 3. van Wijngaarden J, et al. An in vitro model that can distinguish between effects on angiogenesis and on established vasculature: actions of TNP-470, marimastat and the tubulin-binding agent Ang-510. Biochem Biophys Res Commun. 2010 Jan 8;391(2):1161-5. 4. Skipper JB, et al. In vivo efficacy of marimastat and chemoradiation in head and neck cancer xenografts. ORL J Otorhinolaryngol Relat Spec. 2009;71(1):1-5. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.017 ml |
15.087 ml |
30.174 ml |
| 5 mM |
0.603 ml |
3.017 ml |
6.035 ml |
| 10 mM |
0.302 ml |
1.509 ml |
3.017 ml |
| 50 mM |
0.06 ml |
0.302 ml |
0.603 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京