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Eltanexor Z-isomer

Names

[ CAS No. ]:
1642300-78-4

[ Name ]:
Eltanexor Z-isomer

Biological Activity

[Description]:

KPT-8602 Z-isomer is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.IC50：In Vitro: KPT 8602 Z-isomer exhibits different inhibitory effects on Z138, MM15, 3T3 cell lines, with IC50s of 100 nM-50 μM, < 100 nM, > 30 μM, respectively[1]. In Vivo:

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> CRM1
Research Areas >> Cancer

[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.

[2]. Hing ZA et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Jun 21.

[3]. Etchin J 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. 2016 Jun 24.


[Related Small Molecules]

KPT-8602 | KPT 330 | KPT-185 | KPT-276 | Verdinexor

Chemical & Physical Properties

[ Molecular Formula ]:
C17H10F6N6O

[ Molecular Weight ]:
428.29

Related Compounds