別品名 |
Zoledronic acid disodium salt tetrahydrate, [1-Hydroxy-2-(1H-imidazol-1-yl)ethylidene]- bisphosphonic acid disodium salt tetrahydrate
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別包装 |
あり
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純度 |
>=98%
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分子量 |
390.13
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CAS RN® |
165800-07-7
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化合物の概要 |
Bisphosphonate; FPPS inhibitor.
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構造 |
C5H10N2O7P2 2Na+ 4H2O
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使用目的 |
Zoledronate is a sodium salt form of zoledronic acid. Zoledronic acid is a third generation bisphosphonate that exhibits anti-resorptive, anti-osteoporotic, anti-angiogenic, and anticancer chemotherapeutic activities. In giant cell tumor bone stromal cells, zoledronic acid increases expression of Cbfa-1, osteocalcin, and osterix, inducing apoptosis and osteogenic differentiation; it also inhibits bone resorption and prevents osteoporosis in animal models. In animal models of renal cell carcinoma, zoledronic acid decreases mean vessel density. In breast cancer cells, zoledronic acid reverses the epithelial-to-mesenchymal transition (EMT) by inactivating NF-κB, decreasing self-renewal and cell proliferation. In other cellular models, zoledronic acid inhibits farnesyl diphosphate synthase (FPPS), which results in activation of γδ T cells. Across several breast cancer cell lines, zoledronic acid activates caspases 3, 8, and 9 and decreases expression of Ras and MAPK, resulting in the induction of cell cycle arrest or apoptosis.
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その他 |
[融点]305℃-307℃ [外観]White Crystal Powder
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参考文献 |
Yang T, Zheng XF, Li M, et al. Stimulation of osteogenic differentiation in stromal cells of giant cell tumour of bone by zoledronic acid. Asian Pac J Cancer Prev. 2013;14(9):5379-83. PMID: 24175830.Schech AJ, Kazi AA, Gilani RA, et al. Zoledronic acid reverses the epithelial-mesenchymal transition and inhibits self-renewal of breast cancer cells through inactivation of NF-κB. Mol Cancer Ther. 2013 Jul;12(7):1356-66. PMID: 23619300.Idrees AS, Sugie T, Inoue C, et al. Comparison of γδ T cell responses and farnesyl diphosphate synthase inhibition in tumor cells pretreated with zoledronic acid. Cancer Sci. 2013 May;104(5):536-42. PMID: 23387443.Ibrahim T, Mercatali L, Sacanna E, et al. Inhibition of breast cancer cell proliferation in repeated and non-repeated treatment with zoledronic acid. Cancer Cell Int. 2012 Nov 22;12(1):48. PMID: 23173568.Soltau J, Zirrgiebel U, Esser N, et al. Antitumoral and antiangiogenic efficacy of bisphosphonates in vitro and in a murine RENCA model. Anticancer Res. 2008 Mar-Apr;28(2A):933-41. PMID: 18507039.Kavanagh KL, Guo K, Dunford JE, et al The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs. Proc Natl Acad Sci U S A. 2006 May 16;103(20):7829-34. PMID: 16684881.Takahashi H, Kinbara M, Sato N, et al. Nickel allergy-promoting effects of microbial or inflammatory substances at the sensitization step in mice. Int Immunopharmacol. 2011 Oct;11(10):1534-1540. PMID: 21621645.
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メーカー |
品番 |
包装 |
LKT
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Z5645
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100 MG
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※表示価格について
当社在庫 |
なし
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納期目安 |
1週間程度
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保存温度 |
常温
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