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甲磺酸艾瑞布林
产品纠错
CAS号:441045-17-6 | 英文名称:Eribulin Mesilate
分子式 C41H63NO14S
分子量 826
EINECS号 813-106-4
MDL MFCD22572760
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 甲磺酸艾日布林
英文名称 Eribulin Mesylate
CAS号 441045-17-6
分子式 C41H63NO14S
分子量 826.01
EINECS号 813-106-4
物化性质
溶解度 溶于二甲基亚砜
形态 粉末
颜色 白色至米白色
安全信息
生产及用途

甲磺酸艾日布林是一种抗肿瘤药物,可用于治疗转移性乳腺癌患者。

Eribulin mesylate (E7389 mesylate) 是靶向微管 (microtubule) 的抗癌剂,其用于研究转移性乳腺癌。Eribulin mesylate 通过结合微管蛋白和微管来抑制癌细胞的增殖。

Eribulin (1-100 nM; 72 h) inhibits cells proliferation, with IC 50 s of 22.8 and 21.5 nM for LM8 and Dunn cells, respectively.
Eribulin (10-50 nM; 12-72 h) increases early apoptosis significantly after 24 h treatment at the dose of 50 nM in LM8 cells.
Eribulin (10-50 nM; 12-72 h) induces G2/M arrest by 12 h treatment with at the dose of 50 nM, but not by long-term treatment (72 h) with 10 nM in LM8 cells.
Eribulin (1-50 nM; 12 h) does not induce senescence in LM8 cells.
Eribulin (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells.

Cell Proliferation Assay

Cell Line: LM8 cells and Dunn cells
Concentration: 0, 1, 10, 100 nM
Incubation Time: 72 hours
Result: Inhibited cells proliferation in a dose-dependent manner.

Apoptosis Analysis

Cell Line: LM8 cells
Concentration: 0, 10, 50 nM
Incubation Time: 12, 24, 48, 72 hour
Result: Induced early apoptosis after 12 h at the concentration of 50 nM.
Not detected apoptosis at the concentration of 10 nM.

Cell Cycle Analysis

Cell Line: LM8 cells
Concentration: 0, 10, 50 nM
Incubation Time: 12, 24, 48, 72 hour
Result: Induced G2/M arrest by 12 h treatment with 50 nM.
No G2/M arrest was induced by10 nM treatment.

Eribulin (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis of osteosarcoma in mice.
Eribulin (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase.

Animal Model: C3H/HeN mice (4-week-old) are injected LM8 cells
Dosage: 1 mg/kg
Administration: I.v. once a week for 2 weeks
Result: Suppressed primary tumor growth and induced apoptosis in tumor cells. Reduced lung metastasis.
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