| Bioactivity | Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines[1]. | ||||||||||||
| Target | XPO1 | ||||||||||||
| Invitro | KPT-8602 (2-6 nM;EC50s范围在25 ~ 145 nM[1] KPT-8602 (1 nM;[1]。” Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | KPT-8602 (15 mg/kg；口服填喂法；每日给药；共 12 天) 显示出有效的抗淋巴细胞白血病活性[1]。 Animal Model: | ||||||||||||
| Name | Eltanexor | ||||||||||||
| CAS | 1642300-52-4 | ||||||||||||
| Formula | C17H10F6N6O | ||||||||||||
| Molar Mass | 428.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Eltanexor
CAS: 1642300-52-4 F: C17H10F6N6O W: 428.29
Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent a
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