Ibandronate Sodium
Based on 1 publication(s) in Google Scholar
Ibandronate Sodium is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium inhibits tumor cell proliferation (such as ER+ breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis).
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- 純度: 99.89%
- CAS 番号: 138844-81-2
- 分子式: C9H22NNaO7P2
- 分子量:341.21
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Ibandronate Sodium
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生物活性
Ibandronate Sodium (10-6-10-3 M; 3 d) inhibits cell growth in a dose-dependent manner, induces apoptosis, and completely counteractes the pro-proliferative effect of 17β-estradiol in ER+ breast cancer cell lines MCF-7, IBEP-2, and ER- cell line MDA-MB-231[1].
Ibandronate Sodium (1-200 μM; 72 h) inhibits cell viability, activated caspase 3/7 and 8, upregulates the expression of the pro-apoptotic gene FAS, and downregulates the DNA methyltransferase DNMT1 in human U-2 osteosarcoma and mouse CCL-51 breast cancer cells, and FAS siRNA could partially reverse its growth inhibitory effect[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, IBEP-2 (ER+ breast cancer cells), MDA-MB-231 (ER- breast cancer cells)
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Concentration:10-6 M, 10-5 M, 10-4 M, 10-3 M
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Incubation Time:72 h
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Result:Dose-dependent inhibited cell growth with approximate IC50 of 10-4 M for MCF-7 and IBEP-2, and 3×10-4 M for MDA-MB-231.
Significantly reduced cell count by 40.7% compared to control at 10-4 M.
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Cell Line:MCF-7, IBEP-2 (ER+ breast cancer cells), MDA-MB-231 (ER- breast cancer cells)
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Concentration:10-6 M, 10-5 M, 10-4 M, 10-3 M
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Incubation Time:72 h
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Result:Increased apoptosis in MCF-7 cells treated with 10-4 M and 10-3 M ibandronate, with 23.5% and 50.0% apoptotic cells after 5 days, respectively.
Ibandronate (1 μg/kg/day; oral; 1 week of administration/2-6 weeks of withdrawal; 22 weeks-1 year) Sodium effectively prevents castration-induced bone loss in the female ovariectomized (OVX) rat model, maintaines bone mass, bone structure and biomechanical strength, and the effects of intermittent and continuous administration are equivalent[4].
Ibandronate (65 μg/kg/day; oral; 2 weeks on/11 weeks off; 1 year) Sodium dose-dependently increases bone volume in female ovariohysterectomized (OHX) beagle dogs, completely reverses castration-induced bone loss and restores bone density to control levels[4].
Ibandronate (10-150 μg/kg; intravenous injection; once a month; 16 months) Sodium dose-dependently prevents bone loss at the lumbar spine and femoral neck in female ovariectomized cynomolgus monkeys, with the highest dose restoring bone density to sham-operated group levels, and has no adverse effects on bone mineralization and healing[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female HanIbm:Wistar rats (176-214 g, 9 weeks old) in renal safety study[3]
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Dosage:1 mg/kg Ibandronate
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Administration:Intravenous (i.v.) injection, once every 3 weeks, for a total of 9 doses over 25 weeks
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Result:Biochemical Parameters:
Serum creatinine, urea, urinary protein, and enzyme activities (α-GST, LDH, NAG) showed no significant changes compared to control groups. Creatinine clearance remained stable without notable decline.
Histopathology:
Minimal proximal convoluted tubule (PCT) degeneration and single-cell necrosis were observed in 1/6 rats after a single dose and 2/6 rats after intermittent dosing, with severity score 1.0 in both cases. No accumulation of renal damage was detected, and no hypertrophy/hyperplasia of distal tubules or collecting ducts occurred after single dosing, though mild hypertrophy was noted after intermittent dosing.
Comparison with Zoledronate:
In contrast to zoledronate, ibandronate did not exhibit increased renal damage severity or incidence with intermittent dosing, confirming no cumulative nephrotoxicity at this dose.
化学情報
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CAS 番号 138844-81-2
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性状 Solid
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分子量 341.21
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分子式 C9H22NNaO7P2
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Color White to off-white
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SMILES
OC(P(O)(O)=O)(P(O)([O-])=O)CCN(C)CCCCC.[Na+]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Parasitol Drugs Drug Resist
Promising efficacy of nitrogen-containing bisphosphonates against the infection of Cryptosporidium spp. [Abstract]2025 Aug 6:29:100607. PMID: 40782657
溶剤 & 溶解度
H2O : 25 mg/mL (73.27 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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参考文献
[1]. Journe F, et al. Additive growth inhibitory effects of ibandronate and antiestrogens in estrogen receptor-positive breast cancer cell lines. Breast Cancer Res. 2006;8(1):R2. [Content Brief]
[2]. Thaler R, et al. Ibandronate increases the expression of the pro-apoptotic gene FAS by epigenetic mechanisms in tumor cells. Biochem Pharmacol. 2013 Jan 15;85(2):173-85. [Content Brief]
[3]. Pfister T, et al. The renal effects of minimally nephrotoxic doses of ibandronate and zoledronate following single and intermittent intravenous administration in rats. Toxicology. 2003 Sep 30;191(2-3):159-67. [Content Brief]
[4]. Russell RG. Ibandronate: pharmacology and preclinical studies. Bone. 2006 Apr;38(4 Suppl 1):S7-12. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.9307 mL | 14.6537 mL | 29.3075 mL | 73.2687 mL |
| 5 mM | 0.5861 mL | 2.9307 mL | 5.8615 mL | 14.6537 mL | |
| 10 mM | 0.2931 mL | 1.4654 mL | 2.9307 mL | 7.3269 mL | |
| 15 mM | 0.1954 mL | 0.9769 mL | 1.9538 mL | 4.8846 mL | |
| 20 mM | 0.1465 mL | 0.7327 mL | 1.4654 mL | 3.6634 mL | |
| 25 mM | 0.1172 mL | 0.5861 mL | 1.1723 mL | 2.9307 mL | |
| 30 mM | 0.0977 mL | 0.4885 mL | 0.9769 mL | 2.4423 mL | |
| 40 mM | 0.0733 mL | 0.3663 mL | 0.7327 mL | 1.8317 mL | |
| 50 mM | 0.0586 mL | 0.2931 mL | 0.5861 mL | 1.4654 mL | |
| 60 mM | 0.0488 mL | 0.2442 mL | 0.4885 mL | 1.2211 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ibandronate Sodium 関連分類
HY-B0515B 関連分類
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