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来普霉素B;87081-35-4
  • 品牌:Absin
  • 产地:上海
  • 货号:abs823359
  • cas:87081-35-4
  • 价格: ¥4150/瓶
  • 发布日期: 2023-09-14
  • 更新日期: 2024-07-22
产品详请
产地 上海
品牌 Absin
货号 abs823359
用途 -
CAS编号 87081-35-4
纯度 ≥98%%
规格 5mg;10mg
是否进口

描述:Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.

来源:Bacterium/Streptomyces sp

储存/保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

别名:来普霉素B; Elactocin;LMB;Mantuamycin

外观:White to off-white powder

可溶性/溶解性:DMSO : 100 mg/mL (184.94 mM; Need ultrasonic)

靶点:CRM1/exportin 1


In vitro(体外研究):

Leptomycin B (LMB) is very potent in vitro against various cancer cell lines (IC50 values in the 0.1 to 10 nM range). Leptomycin B (LMB) inhibits SiHa, HCT-116, and SKNSH cells with IC50s of 0.4, 0.3 and 0.4 nM for a 72 hour exposure, respectively.
Leptomycin B (LMB) (0.5 nM) displays a synergistic effect on Gefitinib (0–32 μM)-induced cytotoxicity in A549 and H460 cell line. The simultaneous treatments of Gefitinib (0–32 μM) and Leptomycin B (0.5 nM) show synergistic cytotoxic effect on A549 as compared to Gefitinib alone at both 24 and 48 hours.


In vivo(体内研究):

Leptomycin B (LMB) is poorly tolerated in vivo. Maximum tolerated dose (MTD) is 2.5 mg/kg for LMB (single i.v.) in HCT-116 tumor–bearing mice.The limited in vivo efficacy of Leptomycin B is due to off-target effects because our nuclear export inhibitors (NEIs) retain the potent inhibition of CRM1, but are clearly better tolerated in vivo.


实验结果图:


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