Eltanexor

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Chemical Structure| 1642300-52-4 同义名 : KPT-8602; ONO-7706,ATG-016
CAS号 : 1642300-52-4
货号 : A579961
分子式 : C17H10F6N6O
纯度 : 99%+
分子量 : 428.29
MDL号 : MFCD30489739
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • CRM1
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].
实验方案
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
参考文献

[1]Etchin J, Berezovskaya A, 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 Jan;31(1):143-150.

[2]Hing ZA, Fung HY, et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Dec;30(12):2364-2372.