Zoledronic acid (Zoledronate)

製品コードS1314 バッチS131403

化学情報

	Synonyms	ZA, CGP-4244, GP42446A, ZOL 446	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₅H₁₀N₂O₇P₂
	分子量	272.09	CAS No.	118072-93-8
Solubility (25°C)*	体外	0.5MNAOH	6.05 mg/mL (22.23 mM)
		DMSO	0.005 mg/mL (0.01 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
in vitro	Zoledronic acid (Zoledronate) (10 µM and 100 µM) causes a significant reduction in the proportions of MCF-7 cells (49.54% and 23.55% of control, respectively) (P < 0.05). It has little effect on MDA-MB-231 cells at concentrations of 0.1–10 µM, whereas the 100 µM concentration results in a significant reduction in cell number. This compound (100 µM) results in a 63.5% reduction in MCF-7 cell number at 72 hours and an 87.1% reduction at 96 hours. It (10 µM) results in a greater than 4-fold increase in MCF-7 cell apoptosis whereas the 100 µM concentration induces a 6-fold increase in the proportion of apoptotic cells. When combined with paclitaxel (2 µM), it results in a 5-fold increase in apoptosis (774.8% of control) compared to zoledronic acid alone (155.71%) and a 4-fold increase compared to paclitaxel alone (189.68%). Zoledronic acid-induced apoptosis of MCF-7 breast cancer cells can be inhibited by addition of intermediates of the mevalonate pathway, which is consistent with observations in osteoclasts, macrophages and myeloma cells. ^[1] It enhances OPG gene expression and protein secretion by human osteoblasts (hOB) in a dose-dependent fashion with a maximum effect at 10 nM after 72 hours, consistent with the higher biological potency of Zoledronic acid. This compound prevents the inhibitory effects of the glucocorticoid dexamethasone on OPG mRNA and protein production in human osteoblasts. It induces type I collagen secretion and alkaline phosphatase activity by 2- and 4-fold, respectively, in human osteoblasts. ^[2]
in vivo	Zoledronic acid (Zoledronate) (120 ug/kg, s.c.) prevents the formation of lesions, prevents cancellous bone loss and loss of bone mineral density, and reduces osteoclast perimeter in 5T2MM-bearing mice. It (120 mg/kg, s.c.) also decreases paraprotein concentration, decreases tumor burden, and reduces angiogenesis in 5T2MM-bearing mice. ^[3]

製品説明

Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.

in vitro

Zoledronic acid (Zoledronate) (10 µM and 100 µM) causes a significant reduction in the proportions of MCF-7 cells (49.54% and 23.55% of control, respectively) (P < 0.05). It has little effect on MDA-MB-231 cells at concentrations of 0.1–10 µM, whereas the 100 µM concentration results in a significant reduction in cell number. This compound (100 µM) results in a 63.5% reduction in MCF-7 cell number at 72 hours and an 87.1% reduction at 96 hours. It (10 µM) results in a greater than 4-fold increase in MCF-7 cell apoptosis whereas the 100 µM concentration induces a 6-fold increase in the proportion of apoptotic cells. When combined with paclitaxel (2 µM), it results in a 5-fold increase in apoptosis (774.8% of control) compared to zoledronic acid alone (155.71%) and a 4-fold increase compared to paclitaxel alone (189.68%). Zoledronic acid-induced apoptosis of MCF-7 breast cancer cells can be inhibited by addition of intermediates of the mevalonate pathway, which is consistent with observations in osteoclasts, macrophages and myeloma cells. ^[1]

It enhances OPG gene expression and protein secretion by human osteoblasts (hOB) in a dose-dependent fashion with a maximum effect at 10 nM after 72 hours, consistent with the higher biological potency of Zoledronic acid. This compound prevents the inhibitory effects of the glucocorticoid dexamethasone on OPG mRNA and protein production in human osteoblasts. It induces type I collagen secretion and alkaline phosphatase activity by 2- and 4-fold, respectively, in human osteoblasts. ^[2]

in vivo

Zoledronic acid (Zoledronate) (120 ug/kg, s.c.) prevents the formation of lesions, prevents cancellous bone loss and loss of bone mineral density, and reduces osteoclast perimeter in 5T2MM-bearing mice. It (120 mg/kg, s.c.) also decreases paraprotein concentration, decreases tumor burden, and reduces angiogenesis in 5T2MM-bearing mice. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MCF7 cells
	濃度	100 μM
	反応時間	72 h
	実験の流れ	Zoledronic acid (Zoledronate) was used to treat cells at various concentrations for 72 h.
動物実験	動物モデル	Male C57BL/KaLwRij mice
	投薬量	120 µg/kg
	投与方法	s.c.

参考

https://pubmed.ncbi.nlm.nih.gov/11308265/
https://pubmed.ncbi.nlm.nih.gov/11855844/
https://pubmed.ncbi.nlm.nih.gov/12619933/

カスタマーフィードバック

: Data from [Data independently produced by Liver Int, 2013, 33(1), 127-36]

: Data from [Data independently produced by , , J Mol Cell Cardiol, 2016, 99:76-86.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HIF2-driven PTHrP Causes Cachexia and Hypercalcemia in Kidney Cancer: Treatment with HIF2 Inhibitors [ bioRxiv, 2025, 2025.09.09.675147]	PubMed: 40964365
Antibody-Drug Conjugate Made of Zoledronic Acid and the Anti-CD30 Brentuximab-Vedotin Exert Anti-Lymphoma and Immunostimulating Effects [ Cells, 2024, 13(10)862]	PubMed: 38786084
Antibody-Drug Conjugate Made of Zoledronic Acid and the Anti-CD30 Brentuximab-Vedotin Exert Anti-Lymphoma and Immunostimulating Effects [ Cells, 2024, 13(10)862]	PubMed: 38786084
Mechanism exploration of Zoledronic acid combined with PD-1 in the treatment of hepatocellular carcinoma [ Cancer Immunol Immunother, 2024, 73(4):62]	PubMed: 38430249
SLFN12 Expression Significantly Effects the Response to Chemotherapy Drugs in Triple-Negative Breast Cancer [ Cancers (Basel), 2024, 16(22)3848]	PubMed: 39594803
EGFR-Targeted Antibody-Drug Conjugate to Different Aminobisphosphonates: Direct and Indirect Antitumor Effects on Colorectal Carcinoma Cells [ Cancers (Basel), 2024, 16(7)1256]	PubMed: 38610932
Zoledronate interrupts pre-osteoclast-induced angiogenesis via SDF-1/CXCR4 pathway [ Bone Rep, 2024, 23:101812]	PubMed: 39583183
BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism [ Nat Commun, 2023, 14(1):1413]	PubMed: 36918560
BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism [ Nature Communications, 2023, 1413-2023)]	PubMed: None
Priming of Colorectal Tumor-Associated Fibroblasts with Zoledronic Acid Conjugated to the Anti-Epidermal Growth Factor Receptor Antibody Cetuximab Elicits Anti-Tumor Vδ2 T Lymphocytes [ Cancers (Basel), 2023, 15(3)610]	PubMed: 36765569

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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