S80401 |
Marimastat |
源叶(MedMol) | 95% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)