1. Apoptosis
  2. Apoptosis
  3. Ibandronate Sodium

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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Ibandronate Sodium

Ibandronate Sodium Chemical Structure

CAS No. : 138844-81-2

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Based on 1 publication(s) in Google Scholar

Other Forms of Ibandronate Sodium:

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1 Publications Citing Use of MCE Ibandronate Sodium

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1][2][3][4].

In Vitro

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.

Cell Viability Assay[1]

Cell Line: MCF-7, IBEP-2 (ER+ breast cancer cells), MDA-MB-231 (ER- breast cancer cells)
Concentration: 10-6 M, 10-5 M, 10-4 M, 10-3 M
Incubation Time: 72 h
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.

Apoptosis Analysis[1]

Cell Line: MCF-7, IBEP-2 (ER+ breast cancer cells), MDA-MB-231 (ER- breast cancer cells)
Concentration: 10-6 M, 10-5 M, 10-4 M, 10-3 M
Incubation Time: 72 h
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.
In Vivo

Ibandronate (1 mg/kg; intravenous injection; once every 3 weeks; a total of 9 times) Sodium does not cause cumulative renal damage in rats, only induces a mild degree of proximal tubular degeneration and single cell necrosis, and the biochemical parameters are not significantly different from the control group[3].
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.

Animal Model: Female HanIbm:Wistar rats (176-214 g, 9 weeks old) in renal safety study[3]
Dosage: 1 mg/kg Ibandronate
Administration: Intravenous (i.v.) injection, once every 3 weeks, for a total of 9 doses over 25 weeks
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.
Molecular Weight

341.21

Formula

C9H22NNaO7P2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(P(O)(O)=O)(P(O)([O-])=O)CCN(C)CCCCC.[Na+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 25 mg/mL (73.27 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9307 mL 14.6537 mL 29.3075 mL
5 mM 0.5861 mL 2.9307 mL 5.8615 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.89%

References

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.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ibandronate Sodium
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