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Leptomycin B
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Leptomycin B图片
CAS NO:87081-35-4
包装与价格:
包装价格(元)
10ug (solution)电议
25ug (solution)电议

产品介绍

化学性质

Physical AppearanceA solution in ethanol
StorageDesiccate at -20°C
M.Wt540.74
Cas No.87081-35-4
FormulaC33H48O6
SolubilitySoluble in ethanol
Chemical Name(2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-((2S,3S)-3-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)-8-oxononadeca-2,10,12,16,18-pentaenoic acid
Canonical SMILESO[C@@H]([C@H](C)C([C@@H](/C=C(C)/C=C/C[C@@H](C)/C=C(CC)\C=C\[C@@H]([C@H](C=C1)C)OC1=O)C)=O)[C@@H](C)C/C(C)=C/C(O)=O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

Leptomycin B is a highly specific inhibitor of the export protein CRM1, with IC50 values ranging from 0.1 to 10 nM against various cancer cell lines [1].

The exportin CRM1 is absolutely required for the nuclear export of a wide variety of cancer-related “cargo” proteins including p53, c-Abl, and FOXO-3A, cytoplasmic localization of which may result in uncontrolled growth and the onset of disease [1].

In 15 sarcoma cell lines with varied histological backgrounds, Leptomycin B showed tumor inhibitory effects, with the average IC50 of 4.23 nM [2]. In A549 cells, Leptomycin B at the concentration of 50 nM, caused CRM1 to redistribute from the nucleus to the cytoplasm [3].

In SiHa tumor–bearing mice, Leptomycin B (25 mg/kg, i.v., one dose per 7 days, for a total of three doses) only exhibited grow delay effects, which was consistent with the limitedin vivo efficacy previously observed for Leptomycin B. In addition, Leptomycin B was also found to be relatively toxic, compared to the Leptomycin B analog [1].

References:

[1]. Mutka S C, Yang W Q, Dong S D, et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Research, 2009, 69(2): 510-517.

[2]. Qiao Z, Kondo T. Screening of a growth inhibitor library of sarcoma cell lines to identify potent anti-cancer drugs. Journal of Electrophoresis, 2019, 63: 1-7.

[3]. Rahmani K, Dean D A. Leptomycin B alters the subcellular distribution of CRM1 (Exportin 1). Biochem Biophys Res Commun. 2017, 488(2): 253-258.