| Description | Eltanexor (ONO-7706) 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. |
| In vitro | Eltanexor (KPT-8602)（1 nM；16小时）能够诱导白血病细胞系发生凋亡。经过72小时作用，KPT-8602（2-6 nM）降低了白血病细胞系的存活率，其半数有效浓度（EC50）介于25至145 nM之间。 |
| In vivo | KPT-8602（口服灌胃，每天15 mg/kg，连续12天）有效展示了对抗淋巴母细胞性白血病的活性。 |
| Target activity | XPO1:60.9 nM(EC50) |
| Synonyms | ONO-7706, KPT-8602, ATG-016 |
| molecular weight | 428.29 |
| Molecular formula | C17H10F6N6O |
| CAS | 1642300-52-4 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 80 mg/mL (186.78 mM) H2O: < 0.1 mg/mL (insoluble) |
| References | 1. Vercruysse T et al. The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. Clin Cancer Res. 2016 Oct 25. |