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441045-17-6

中文名稱 甲磺酸艾日布林
英文名稱 Eribulin Mesylate
CAS 441045-17-6
分子式 C40H59NO11.CH4O3S
分子量 826.01
MOL 文件 441045-17-6.mol
更新日期 2025/01/24 00:06:54
441045-17-6 結構式 441045-17-6 結構式

基本信息

中文別名
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
英文別名
Halaven
E7389 mesylate
B1939 mesylate
Eribulin Mesylate
Eribulin Mesilate
ER-086526 mesylate
EribulinMesylate USP/EP/BP
Eribulin mesylate Halaven
所屬類別
原料藥:其它抗腫瘤藥

物理化學性質

儲存條件Store at -20°C, protect from light, stored under nitrogen
溶解度溶于二甲基亞砜
形態(tài)粉末
顏色White to off-white
InChIKeyQAMYWGZHLCQOOJ-PEKQNERQNA-N

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

應用

甲磺酸艾日布林是一種抗腫瘤藥物,可用于治療轉移性乳腺癌患者。

生物活性
Eribulin mesylate (E7389 mesylate) 是靶向微管 (microtubule) 的抗癌劑,其用于研究轉移性乳腺癌。Eribulin mesylate 通過結合微管蛋白和微管來抑制癌細胞的增殖。
體外研究

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.
體內研究

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.
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