Zoledronic acid (Zoledronate)

製品コードS1314 バッチS131405

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	0.1M NAOH	25 mg/mL (91.88 mM)
		Water	0.5 mg/mL (1.83 mM)
		DMSO	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.

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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 (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). Zoledronic acid 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. Zoledronic acid (100 µM) results in a 63.5% reduction in MCF-7 cell number at 72 hours and an 87.1% reduction at 96 hours. Zoledronic acid (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. Zoledronic acid (10 µM) and paclitaxel (2 µM) 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] Zoledronic acid 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. Zoledronic acid prevents the inhibitory effects of the glucocorticoid dexamethasone on OPG mRNA and protein production in human osteoblasts. Zoledronic acid induces type I collagen secretion and alkaline phosphatase activity by 2- and 4-fold, respectively, in human osteoblasts. ^[2]
in vivo	Zoledronic acid (120 mg/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. Zoledronic acid (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 (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). Zoledronic acid 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. Zoledronic acid (100 µM) results in a 63.5% reduction in MCF-7 cell number at 72 hours and an 87.1% reduction at 96 hours. Zoledronic acid (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. Zoledronic acid (10 µM) and paclitaxel (2 µM) 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]

Zoledronic acid 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. Zoledronic acid prevents the inhibitory effects of the glucocorticoid dexamethasone on OPG mRNA and protein production in human osteoblasts. Zoledronic acid induces type I collagen secretion and alkaline phosphatase activity by 2- and 4-fold, respectively, in human osteoblasts. ^[2]

in vivo

Zoledronic acid (120 mg/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. Zoledronic acid (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	Cells were treated with various concentrations of drug 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

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：

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
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
γδ-Enriched CAR-T cell therapy for bone metastatic castrate-resistant prostate cancer [ Sci Adv, 2023, 9(18):eadf0108]	PubMed: 37134157
Select HDAC Inhibitors Enhance Osteolysis and Bone Metastasis Outgrowth but Can Be Mitigated With Bisphosphonate Therapy [ JBMR Plus, 2023, 7(3):e10694]	PubMed: 36936362
Zoledronic Acid Inhibits the Growth of Breast Malignant Phyllodes Tumor by Inducing Mitotic Catastrophe Via the Plk1 Signaling Pathway [ SSRN, 2023, 38 Pages]	PubMed: none
Targeting of colorectal cancer organoids with zoledronic acid conjugated to the anti-EGFR antibody cetuximab [ J Immunother Cancer, 2022, 10(12)e005660]	PubMed: 36543375
Label-free metabolic imaging for sensitive and robust monitoring of anti-CD47 immunotherapy response in triple-negative breast cancer [ J Immunother Cancer, 2022, 10-9e005199]	PubMed: 36096527
Label-free metabolic imaging for sensitive and robust monitoring of anti-CD47 immunotherapy response in triple-negative breast cancer [ J Immunother Cancer, 2022, 10-9e005199]	PubMed: 36096527

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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