产品说明书

Zoledronic Acid

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Chemical Structure| 118072-93-8 同义名 : Zoledronate;CGP42446A;GP42446A;CGP-4244;ZA;ZOL 446;CGP 42446
CAS号 : 118072-93-8
货号 : A364741
分子式 : C5H10N2O7P2
纯度 : 98%
分子量 : 272.09
MDL号 : MFCD00867791
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 5 mg/mL(18.38 mM)，配合低频超声，水浴加热至45℃，并调节pH至6
动物实验配方：

PO 0.5% CMC-Na 18 mg/mL suspension

生物活性
靶点

  • Rho-subclass
描述 Zoledronic Acid is an intravenous, highly potent aminobisphosphonate approved worldwide, nitrogen-containing bisphosphonate. It is widely used in patients with osteoporosis or low bone mass to prevent or treat osteoporosis[1]. Zoledronic acid once yearly for up to 3 years in patients with primary or secondary osteoporosis significantly improved bone mineral density (BMD), reduced fracture risk and bone turnover. When treatment was continued for up to 6 years, additional benefits were seen, as evidenced by a reduced risk of vertebral fractures and higher BMD relative to 3 years' therapy. Zoledronic acid is also approved by FDA in 2007 for the treatment of postmenopausal osteoporosis[2]. Moreover, data from in vitro and pilot studies suggest that zoledronic acid also has antitumor activity including multiple myeloma and solid tumors with bone metastases. In vitro, 5.0 µmol/L zoledronic acid significantly inhibit HGF proliferation and promote its apoptosis rate[3]. In animal models, Zoledronic acid combination with anticancer therapies can increases apoptosis, inhibits tumor cell proliferation, and enhances immune surveillance[4]. Early studies of bone metastases have showed that low-dose zoledronic acid (30 μg/kg subcutaneous) can directly inhibit melanoma tumor bone growth in mice. In KRAS mutant cancers, it can enhance the efficacy of the MEK inhibitor trametinib, and disrupt the biological activity of RAS by suppressing its isoprenylation[5]. Zoledronic acid used along with cancer radiotherapy significantly decreased bone pain and improved the mean quality of life (QOL) in treating painful bone metastases from gastrointestinal cancers[6].
作用机制 Zoledronic Acid is an intravenous, highly potent aminobisphosphonate.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human foreskin fibroblast monolayer cells (HFF cells) Growth inhibition assay In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells), IC50=0.79 μM 15857119
human Gamma delta T cells Function assay Effective concentration against human Gamma delta T cells, EC50=5.4 μM 15828834
human MCF7 cells Proliferation assay 72 h Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=23 μM 24928399
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.68mL

0.74mL

0.37mL

18.38mL

3.68mL

1.84mL

36.75mL

7.35mL

3.68mL
参考文献

[1]Dhillon S. Zoledronic Acid (Reclast®, Aclasta®): A Review in Osteoporosis. Drugs. 2016;76(17):1683-1697.

[2]Miller PD, Pannacciulli N, et al. Denosumab or Zoledronic Acid in Postmenopausal Women With Osteoporosis Previously Treated With Oral Bisphosphonates. J Clin Endocrinol Metab. 2016;101(8):3163-70.

[3]Fu Q, Cui C, et al. [Effect of zoledronic acid on cell proliferation and apoptosis of human periodontal fibroblasts]. Zhonghua Kou Qiang Yi Xue Za Zhi. 2015;50(11):667-70.

[4]Green J, Lipton A. Anticancer properties of zoledronic acid. Cancer Invest. 2010;28(9):944-57.

[5]Dai X, Xia H, et al. Zoledronic acid enhances the efficacy of the MEK inhibitor trametinib in KRAS mutant cancers. Cancer Lett. 2019.

[6]Choi J, Lee EJ, et al. A prospective Phase II study for the efficacy of radiotherapy in combination with zoledronic acid in treating painful bone metastases from gastrointestinal cancers. J Radiat Res. 2018.