甲磺酸艾日布林

中文名称:

甲磺酸艾日布林

中文同义词:

甲磺酸艾瑞布林;艾瑞布林/甲磺酸艾瑞布林/甲磺酸艾日布林/艾日布林

英文名称:

Eribulin Mesylate

英文同义词:

Eribulin Mesylate;Halaven;Eribulin mesylate Halaven;Eribulin Mesilate;ER-086526 mesylate;B1939 mesylate;E7389 mesylate;EribulinMesylate USP/EP/BP

CAS号:

441045-17-6

分子式:

C41H63NO14S

分子量:

826.01

EINECS号:

813-106-4

相关类别:

医药原料药-科研原料;原料药;抑制剂;API;API

Mol文件:

441045-17-6.mol

应用

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。

生物活性

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。

体外研究

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.

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.

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 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.

体内研究

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.

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.