Eltanexor (KPT-8602)
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mg | ￥413.00 | 现货 | |
| 5mg | ￥1615.00 | 现货 | |
| 10mg | ￥2380.00 | 现货 | |
| 50mg | ￥6426.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
Eltanexor (KPT-8602) is a second-generation, orally bioavailable inhibitor of exportin 1 (XPO1), with IC50 values of 20 ~ 211 nM in 10 acute myeloid leukemia (AML) cell lines. XPO1, also known as chromosome maintenance protein 1 (CRM1), is an important nuclear-cytoplasmic exporter in eukaryotes that transports a variety of protein cargoes from the nucleus to the cytoplasm, such as tumor suppressor proteins, cell cycle regulators and apoptosis inducers. Inhibition of XPO1-mediated nuclear export is a promising therapeutic strategy for many cancers, including chronic lymphocytic leukemia (CLL), AML, and aggressive lymphomas.
References:
1. Etchin J, Berezovskaya A, Conway AS, et al. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia, 2017, 31(1): 143-150.
2. Hing ZA, Fung HY, Ranganathan P, et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia, 2016, 30(12): 2364-2372.
产品性质
| 物理外观 | A solid |
| CAS号 | 1642300-52-4 |
| 分子式 | C17H10F6N6O |
| 分子量 | 428.29 |
| 小分子别名 | Eltanexor |
| 化学名称 | (E)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-2-(pyrimidin-5-yl)acrylamide |
| 溶解度 | insoluble in H2O; insoluble in EtOH; ≥44 mg/mL in DMSO |
| SMILES | NC(/C(\c1cncnc1)=C/[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | Eltanexor（KPT-8602）是第二代高特异性口服活性导出素-1（XPO1）抑制剂，具有强大的抗白血病活性。Eltanexor (KPT-8602)通过直接靶向XPO1，抑制XPO1依赖性核输出（EC50=60.9 nM）。Eltanexor (KPT-8602)能诱导白血病细胞系中的Caspase依赖性凋亡。 |
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