货号:A579961 同义名: KPT-8602;ONO-7706,ATG-016
KPT-8602 is a second-generation and oral acitve exportin-1 (XPO1/CRM1) inhibitor with IC50 of 20−211 nM in 10 AML cell lines.
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产品名称 | CRM1 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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KPT-185 | ✔ | 98+% | |||||||||||||||||
Verdinexor | ✔ | 99%+ | |||||||||||||||||
KPT-276 | ✔ | 99%+ | |||||||||||||||||
Selinexor | ✔ | 99%+ | |||||||||||||||||
Piperlongumine | ✔ | 99%+ | |||||||||||||||||
Eltanexor | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
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描述 | Eltanexor, also known as KPT-8602, is a second-generation, orally administered inhibitor that is highly selective for exportin-1 (XPO1), exhibiting strong anti-leukemic properties. It effectively blocks XPO1-dependent nuclear export with an EC50 of 60.9 nM by directly interacting with XPO1.Eltanexor, administered at concentrations between 2 and 6 nM for a duration of 72 hours, diminishes cell viability in leukemia cell lines, with EC50 values spanning from 25 to 145 nM. Also, it triggers apoptosis in leukemia cell lines[1]. |
Animal study | Administered through oral gavage at a dose of 15 mg/kg daily for 12 days, KPT-8602 exhibits strong activity against lymphoblastic leukemia[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.33mL 0.47mL 0.23mL |
11.67mL 2.33mL 1.17mL |
23.35mL 4.67mL 2.33mL |
CAS号 | 1642300-52-4 |
分子式 | C17H10F6N6O |
分子量 | 428.291 |
别名 | KPT-8602;ONO-7706,ATG-016;eltanexor [INN];Eltanexor [WHO-DD];ELTANEXOR [USAN] |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 105 mg/mL(245.16 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |