2. Apoptosis
  3. Apoptosis
  4. 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 Chemical Structure

Ibandronate Sodium Chemical Structure

CAS No. : 138844-81-2

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Ibandronate Sodium Related Antibodies

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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.

Ibandronate Sodium Related Antibodies

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.
Clinical Trial
Molecular Weight

341.21

Formula

C9H22NNaO7P2
CAS No.
SMILES

OC(P(O)(O)=O)(P(O)([O-])=O)CCN(C)CCCCC.[Na+]
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Room temperature in continental US; may vary elsewhere.
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References
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Ibandronate Sodium Related Classifications

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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.

Keywords:

Ibandronate138844-81-2ApoptosisInhibitorinhibitorinhibit

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