Eltanexor 是一种具有口服活性的 exportin-1 (XPO1) 抑制剂。它具有有效的抗白血病活性。 Eltanexor 通过直接靶向 XPO1 抑制 XPO1 依赖性核输出 (EC50=60.9 nM)。 Eltanexor 在一组白血病细胞系中引起半胱天冬酶依赖性细胞凋亡。

Eltanexor is an orally active exportin-1 (XPO1) inhibitor. It has effective anti-leukemic activity. Eltanexor inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor causes caspase-dependent apoptosis in a panel of leukemic cell lines.

Eltanexor (KPT-8602) (1 nM; 16 hours) causes apoptosis in leukemia cell lines. KPT-8602 (2-6 nM; 72 hours) decreases cell viability in leukemia cell lines (EC50s ranging from 25 to 145 nM).

KPT-8602 (15 mg/kg; oral gavage; daily for 12 days) displays effective anti-lymphoblastic leukemia activity.

1642300-52-4

C17H10F6N6O

428.29

KPT-8602;ONO-7706;ATG-016

H2O:< 0.1 mg/mL (insoluble)
DMSO:80 mg/mL (186.78 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years