1. Apoptosis
  2. Apoptosis
  3. Ibandronate Sodium

Ibandronate Sodium  (Synonyms: 伊班膦酸钠)

目录号: HY-B0515B
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Ibandronate Sodium 是一种口服有效、选择性的法尼基焦磷酸合酶 (FPP synthase) 的抑制剂。Ibandronate Sodium 可阻断甲羟戊酸途径抑制小 GTP 酶 (如 RAS、RHO 家族蛋白) 的异戊二烯化修饰,诱导肿瘤细胞凋亡并抑制骨吸收。Ibandronate Sodium 抑制肿瘤细胞增殖 (如 ER+ 乳腺癌细胞)、促进促凋亡基因 FAS 表达,并可与抗雌激素化合物产生协同抗肿瘤效应。Ibandronate Sodium 用于骨质疏松、骨转移性肿瘤 (如乳腺癌骨转移) 的研究。

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Ibandronate Sodium

Ibandronate Sodium Chemical Structure

CAS No. : 138844-81-2

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Other Forms of Ibandronate Sodium:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Ibandronate Sodium (10-6-10-3 M;3 d) 在 ER+ 乳腺癌细胞系 MCF-7、IBEP-2 及 ER- 细胞系 MDA-MB-231 中呈剂量依赖性抑制细胞生长,诱导凋亡并完全抵消 17β-雌二醇的促增殖作用[1]
Ibandronate Sodium (1-200 μM;72 h) 在人 U-2 骨肉瘤和小鼠 CCL-51 乳腺癌细胞中抑制细胞活力,激活 caspase 3/7 和 8,上调促凋亡基因 FAS 表达并下调 DNA 甲基转移酶 DNMT1,且 FAS siRNA 可部分逆转其生长抑制作用[2]

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.
体内研究
(In Vivo)

Ibandronate (1 mg/kg;静脉注射;每 3 周 1 次;共 9 次) Sodium 不导致大鼠的肾损伤累积,仅诱导轻微程度的近端肾小管变性和单细胞坏死,且生化参数与对照组无显著差异[3]
Ibandronate (1 μg/kg/day;口服;1 周给药/2-6 周停药;22 周-1 年) Sodium 在雌性卵巢切除 (OVX) 大鼠模型中有效预防去势诱导的骨丢失,维持骨量、骨结构及生物力学强度,且间歇与连续给药效果相当[4]
Ibandronate (65 μg/kg/day;口服;2 周给药/11 周停药;1 年) Sodium 在雌性卵巢子宫切除 (OHX) 比格犬模型中剂量依赖性增加骨体积,完全逆转去势诱导的骨丢失并恢复骨密度至对照组水平[4]
Ibandronate (10-150 μg/kg;静脉注射;每月 1 次;16 个月) Sodium 在雌性卵巢切除食蟹猴模型中剂量依赖性防止腰椎及股骨颈骨丢失,最高剂量使骨密度恢复至假手术组水平,且未对骨矿化与愈合产生不良影响[4]

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.
分子量

341.21

Formula

C9H22NNaO7P2

CAS 号
中文名称

伊班膦酸钠;伊班磷酸钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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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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HY-B0515B
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