产品说明
一般描述
An amino-bisphosphonate that acts as a potent inhibitor of bone resorption and cartilage destruction. Causes disruption of the ruffled border and actin cytoskeleton of osteoclasts and induces in vitro apoptosis of osteoclasts and macrophages by inhibiting farnesyl diphosphate synthase (IC50 = 460 nM). Efficiently chelates metal ions and functions as a broad-spectrum MMP inhibitor (IC50 ~ 40 - 70 µM). Also displays antimetastatic, anti-invasive and cell-adhesion-promoting properties (IC50 ~ 1 pM, in vitro invasion of prostate cancer cells).
An amino-bisphosphonate that acts as a potent inhibitor of bone resorption and cartilage destruction. Causes disruption of the ruffled border and actin cytoskeleton of osteoclasts. Shown to induce apoptosis of osteoclasts and macrophages. Inhibits farnesyl disphosphate synthase (IC50 = 460 nM with purified enzyme and 1.7 µM with cell extracts). Also shown to inhibit migration, cell adhesion, and invasion of cells (IC50 = 1 pM in prostate cancer cell invasion assays). Efficiently chelates metal ions and functions as a matrix metalloprotease (MMP) inhibitor (IC50 = 40-70 µM).
包装
100 mg in Plastic ampoule
生化/生理作用
Target IC50: 460 nM against farnesyl diphosphate synthase; ~ 40 - 70 µM as as a broad-spectrum MMP inhibitor; ~ 1 pM against in vitro invasion of prostate cancer cells
Primary Target
Farnesyl diphosphate synthase
Product does not compete with ATP.
Reversible: no
Cell permeable: no
警告
Toxicity: Harmful (C)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Lehenkari, P.P., et al. 2002. Mol. Pharmacol.62, 1255.
Virtanen, S.S., et al. 2002. Cancer Res.62, 2708.
Bergstrom, J.D., et al. 2000. Arch. Biochem. Biophys.373, 231.
Smith, R., et al. 1971. Lancet1, 945.
Fleisch, H., et al. 1969. Nature223, 211.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C4H12NNaO7P2 · 3H2O |
| 分子量 | 325.12 |
| MDL编号 | MFCD01748233 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (titration) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze desiccated (hygroscopic) |
| 颜色 | white |
| 溶解性 | water: 10 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
安全信息
| 象形图 |  |
| 警示用语： | Warning |
| 危险声明 | H302 |
| 预防措施声明 | P264 - P270 - P301 + P312 - P501 |
| 危险分类 | Acute Tox. 4 Oral |
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
