甲磺酸艾瑞布林

应用生物活性体外研究体内研究甲磺酸艾瑞布林试剂级价格

甲磺酸艾瑞布林

CAS号:441045-17-6
英文名:Eribulin Mesylate
中文名:甲磺酸艾瑞布林
CBNumber:CB00130262
分子式:C41H63NO14S
分子量:826.01
MOL File:441045-17-6.mol

甲磺酸艾瑞布林化学性质

储存条件 :Store at -20°C, protect from light, stored under nitrogen
溶解度 :Soluble in DMSO
形态 :Powder
颜色 :White to off-white
InChIKey :QAMYWGZHLCQOOJ-PEKQNERQNA-N

甲磺酸艾瑞布林性质、用途与生产工艺

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.

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.