Zoledronic Acid
(Synonyms: 唑来膦酸; Zoledronate; CGP 42446; CGP42446A; ZOL 446) 目录号 : GC14701
A bisphosphonate that inhibits bone resorption
Cas No.:118072-93-8
Sample solution is provided at 25 µL, 10mM.
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Zoledronic Acid is a third-generation, nitrogen-containing bisphosphonate, inhibits osteoclast-mediated bone resorption, and also has antitumor activity.
Zoledronic Acid induces apoptosis in HGF and HaCaT cells at 0.5 μM, and causes cell death at 1-5 μM[1]. Zoledronic Acid (50, 100 μM) causes dose- and time-dependent apoptosis in CNE-2Z cells after treatment for 24, 48, and 72 h. Zoledronic Acid (50 μM) also increases the level of ROS, which is supposed to mediate Cl- currents activation in CNE-2Z cells. Furthermore, the apoptosis and chloride currents induced by Zoledronic Acid can be blocked by knocking down ClC-3 protein expression[2].
References:
[1]. Scheper M, et al. A novel soft-tissue in vitro model for bisphosphonate-associated osteonecrosis. ibrogenesis Tissue Repair. 2010 Apr 1;3:6.
[2]. Wang L, et al. The apoptotic effect of Zoledronic acid on the nasopharyngeal carcinoma cells via ROS mediated chloride channel activation. Clin Exp Pharmacol Physiol. 2018 Jun 8.
| Cell experiment [1]: | |
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Cell lines |
The human breast carcinoma cell lines (MCF-7 and MDA-MB-231) |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1–100 μM for 72 hours. |
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Applications |
Treatment of MCF-7 cells with a range of zoledronic acid concentrations had little effect on apoptosis at 0.1 and 1.0 μM, however, an increase in the proportion of apoptotic cells was observed with 10 μM and 100 μM zoledronic acid compared with control (28.7% and 70.7% vs 22.57%, respectively).Treatment of MDA-MB-231 cells with 0.1–1 μM zoledronic acid did not cause an increase in apoptosis, but treatment with the 10 and 100 μM zoledronic acid resulted in a significant increase in the proportions of apoptotic cells (126.6% and 126.6% of control). A significant time-dependent increase in MCF7 cell apoptosis was confirmed when cells were incubated with 100 μM zoledronic acid for 24–96 hours. |
| Animal experiment [2]: | |
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Animal models |
The 5T2MM murine model (Male, 6-week-old, C57BL/KaLwRijHsd mice) |
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Dosage form |
120 g/kg, subcutaneously (sc), twice weekly, 12 weeks. |
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Application |
Treatment of mice bearing 5T2MM cells with zoledronic acid clearly prevented the development of osteolytic bone disease, decreased tumor burden in bone, and increased survival in a model of established myeloma. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Jagdev SP, Coleman RE, Shipman CM , et al .The bisphosphonate, zoledronic acid, induces apoptosis of breast cancer cells: evidence for synergy with paclitaxel. Br J Cancer. 2001 Apr 20;84(8):1126-34. [2] Croucher PI, De Hendrik R, Perry MJ, et al. Zoledronic Acid Treatment of 5T2MM-Bearing Mice Inhibits the Development of Myeloma Bone Disease: Evidence for Decreased Osteolysis, Tumor Burden and Angiogenesis, and Increased Survival .J Bone Miner Res. 2003 Mar;18(3):482-92 | |
| Cas No. | 118072-93-8 | SDF | |
| 别名 | 唑来膦酸; Zoledronate; CGP 42446; CGP42446A; ZOL 446 | ||
| 化学名 | (1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid | ||
| Canonical SMILES | C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O | ||
| 分子式 | C5H10N2O7P2 | 分子量 | 272.09 |
| 溶解度 | ≥ 6.8mg/mL in Water with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6753 mL | 18.3763 mL | 36.7525 mL |
| 5 mM | 0.7351 mL | 3.6753 mL | 7.3505 mL |
| 10 mM | 0.3675 mL | 1.8376 mL | 3.6753 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet