Zoledronic Acid

A bisphosphonate that inhibits bone resorption

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25mg

￥425.00

340.00

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1100.00

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货号: ajci13644
CAS: 118072-93-8
别名: 唑来膦酸; Zoledronate; CGP 42446; CGP42446A; ZOL 446
分子式: C5H10N2O7P2
分子量: 272.09
纯度: >98%
溶解度: ≥ 6.8mg/mL in Water with gentle warming
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.

Protocol

Cell experiment [1]:
Cell lines	The human breast carcinoma cell lines (MCF-7 and MDA-MB-231)
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.
Reacting condition	0.1–100 μM for 72 hours.
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]:
Animal models	The 5T2MM murine model (Male, 6-week-old, C57BL/KaLwRijHsd mice)
Dosage form	120 g/kg, subcutaneously (sc), twice weekly, 12 weeks.
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.
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.
参考文献: [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