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;甲磺酸艾日布林科研试剂;253128-41-5(游离碱)艾日布林及其中间体;甲磺酸艾立布林(GMP);甲磺酸艾立布林;艾日布林甲磺酸盐;甲磺酸艾日布林杂质 |
| 英文名称 | Eribulin Mesylate |
| 英文同义词 | Eribulin Mesylate;Eribulin mesylate Halaven;ER-086526 mesylate;B1939 mesylate;E7389 mesylate;EribulinMesylate USP/EP/BP;Eribulin Mesylate (E7389);Halaven |
| 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;化学试剂;原料药及中间体;API;API;医药原料;医用原料 |
| Mol文件 | 441045-17-6.mol |
| 结构式 |  |
甲磺酸艾日布林 性质
| 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| InChIKey | QAMYWGZHLCQOOJ-PEKQNERQNA-N |
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.
|
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-13442A | 甲磺酸艾日布林 Eribulin mesylate | 441045-17-6 | 500μg | 1860元 |
| 2024/01/25 | HY-13442A | 甲磺酸艾日布林 Eribulin mesylate | 441045-17-6 | 1mg | 2600元 |