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Zoledronic acid monohydrate

別名：zoledronate monohydrate, CGP-4244 monohydrate

窒素含有ビスホスホネートであるZoledronic acid monohydrate（ゾレドロネート、CGP-4244）は、メバロン酸経路の酵素を阻害し、RasやRhoなどの小型GTP結合タンパク質のイソプレニル化を妨げることにより、破骨細胞のアポトーシスを誘発する強力な破骨細胞阻害剤です。

Zoledronic acid monohydrate化学構造

CAS No. 165800-06-6

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 55500 国内在庫なし(納期7~10日)

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製品安全説明書

現在のバッチを見る： S524401 0.5MNAOH] 6.02 mg/mL] false] Water] 2.3 mg/mL] false] DMSO] 0.01 mg/mL] false 純度： 98%
98

Zoledronic acid monohydrate関連製品

Ras阻害剤の選択性比較

生物活性

製品説明 窒素含有ビスホスホネートであるZoledronic acid monohydrate（ゾレドロネート、CGP-4244）は、メバロン酸経路の酵素を阻害し、RasやRhoなどの小型GTP結合タンパク質のイソプレニル化を妨げることにより、破骨細胞のアポトーシスを誘発する強力な破骨細胞阻害剤です。
Targets
Ras Rho
In Vitro
In vitro Zoledronic acid inhibits osteoclast maturation indirectly by increasing OPG protein secretion and decreasing transmembrane RANKL expression in human osteoblasts. Treatment of primary human OB‐like cells with the potent nitrogen-containing BP, zoledronic acid (ZOL), resulted in a downregulation of membrane-ssociated RANKL protein expression. In addition to direct effects on cells of the osteoclast lineage, zoledronic acid may inhibit bone resorption by reducing transmembrane RANKL expression and increasing OPG secretion in osteoclast (OB)-like cells. Zoledronic acid induces growth inhibition (IC50:10–50 μM) and apoptotic death of human pancreatic cancer cells. The proapoptotic effect was correlated to cleavage/activation of caspase-9 and poly(ADP)-ribose polymerase, but not of caspase-3. It interferes with growth and survival pathways downstream to p21ras. Zoledronic acid is also a potent inhibitor of angiogenesis. In vitro, zoledronic acid inhibits proliferation of human endothelial cells stimulated with fetal calf serum, basic fibroblast growth factor (bFGF), and vascular endothelial growth factor (IC50 values 4.1, 4.2, and 6.9 μM, respectively), and modulates endothelial cell adhesion and migration. In cultured aortic rings and in the chicken egg chorioallantoic membrane assay, zoledronic acid reduces vessel sprouting. ZOL also exerted a concentration-dependent, biphasic effect on the adhesion and migration of HUVEC in vitro. ZOL concentrations of 1 and 3 μM increased cell adhesion but inhibited it at 30 and 100 μM. Similarly, cell migration was stimulated by 0.3 to 10 μM ZOL, whereas 30 μM completely inhibited it. These findings suggest that ZOL could interfere with cytoskeletal function in endothelial cells.
細胞実験 細胞株 human PC cell lines (BxPC-3, CFPAC-1 and PANC-1)
濃度 1-100 μM
反応時間 72 h
実験の流れ

'BxPC-3 and CFPAC-1 are adherent human pancreatic adenocarcinoma cell lines that were grown in RPMI 1640 and Iscove's modified Dulbecco's media, respectively. PANC-1 is a human epithelioid pancreas carcinoma cell line that was grown in Dulbecco's modified Eagle's medium (DMEM). All media were supplemented with 10% heat-inactivated fetal bovine serum, 2 mM L-glutamine, 100 μg/ml streptomycin and 100 U/ml penicillin. All PC cell lines were cultured at a constant temperature of 37°C in a humidified atmosphere of 5% carbon dioxide (CO2). The neutralised sodium salt of ZOL was dissolved in sterile ddH2O and used at a final concentration in a range of 1-100 μM. Analysis of cell proliferation was performed on PC cells in the presence of increasing concentrations of ZOL by the MTT assay. Briefly, PC cells (3 × 104/well) were seeded in 96-well plates in serum-containing media and allowed to attach for 24 h. The medium was then removed and replaced with new medium containing ZOL at different concentrations. Cells were incubated under these conditions for a time course spanning 72 h. Then cells were incubated with 10 μl well−1 of thiazolyl blue (MTT, 5 mg/ml) for 1 h at 37°C. After incubation, 100 μl of 0.04 N HCl in isopropanol was added into each well and the absorbance was measured at a wavelength of 620 nm in a microplate reader.
In Vivo
In Vivo Zoledronic acid affects breast cancer metastasis to visceral organs as well as bone. When administered systemically to mice, zoledronic acid potently inhibits the angiogenesis induced by subcutaneous implants impregnated with bFGF [ED50, 3 μg/kg (7.5 nmol/kg) s.c.]. In nice transplanted with osteosarcoma (OS) cells, ZOL administration prevented osteolysis and significantly reduced the amount of OS-induced bone formation while has no effect on tumor burden at the primary site. ZOL failed to reduce lung metastasis and in some cases was associated with larger and more numerous metastatic lesions.
動物実験 動物モデル Female mice (strain Tiflbm:MAG)
投与量 1, 10 and 100 μg/kg
投与経路 s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06374459 RECRUITING
Hormone Receptor Positive HER-2 Negative Metastatic Breast Cancer
Washington University School of Medicine
 2025-01-30 PHASE1; PHASE2
NCT06767150 RECRUITING
Postmenopausal Osteoporosis
University Hospital, Toulouse
 2025-10-02 PHASE4
NCT07406685 RECRUITING
Postmenopausal Osteoporosis; Postmenopausal Osteopenia; Primary Osteoporosis; Osteoporosis
National Taiwan University Hospital
 2026-08-20 PHASE4
NCT06625190 RECRUITING
Neuroblastoma; Rhabdomyosarcoma; Synovial Sarcoma; Peripheral Nerve Sheath Tumors; Clear Cell Sarcoma; Alveolar Soft Part Sarcoma; Desmoplastic Small Round Cell Tumor; Chordoma; Rhabdoid Tumor; Epithelioid Sarcoma; Myoepithelial Tumor; Osteosarcoma; Ewing Sarcoma; Wilms Tumor
University of Florida
 2026-02-11 PHASE1; PHASE2
NCT07772609 NOT_YET_RECRUITING
Osteoporosis in Post-menopausal Women
Sahlgrenska University Hospital
 2027-01-11 PHASE4
NCT07668583 NOT_YET_RECRUITING
Osteomyelitis Chronic
Assistance Publique - Hôpitaux de Paris
 2026-09-15 PHASE2
  • https://pubmed.ncbi.nlm.nih.gov/14753746/
  • https://pubmed.ncbi.nlm.nih.gov/12799645/
  • https://pubmed.ncbi.nlm.nih.gov/15240548/
  • https://pubmed.ncbi.nlm.nih.gov/12183663/
  • https://pubmed.ncbi.nlm.nih.gov/19401351/

化学情報

分子量 290.1 化学式

C5H10N2O7P2.H2O
CAS No. 165800-06-6 SDF --
Smiles C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O.O
保管

In vitro
Batch:

0.5MNAOH : 6.02 mg/mL

Water : 2.3 mg/mL

DMSO : 0.01 mg/mL ( (0.03 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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