| CAS NO: | 87081-35-4 |
| 包装 | 价格(元) |
| 10ug (solution) | 电议 |
| 25ug (solution) | 电议 |
| Physical Appearance | A solution in ethanol |
| Storage | Desiccate at -20°C |
| M.Wt | 540.74 |
| Cas No. | 87081-35-4 |
| Formula | C33H48O6 |
| Solubility | Soluble 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 SMILES | O[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。 |
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.
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