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1642300-78-4

1642300-78-4 Structure

1642300-78-4 Structure
IdentificationBack Directory
[Name]

KPT-8602 (Z-isomer)
[CAS]

1642300-78-4
[Synonyms]

Eltanexor Z-isomer
KPT-8602 (Z-isomer)
Eltanexor Z isomer,Eltanexor Zisomer
KPT-8602 Z-isomer (Eltanexor Z-isomer)
(~{Z})-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-2-pyrimidin-5-ylprop-2-enamide
5-Pyrimidineacetamide, α-[[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]methylene]-, (αZ)-
[Molecular Formula]

C17H10F6N6O
[MDL Number]

MFCD30489756
[MOL File]

1642300-78-4.mol
[Molecular Weight]

428.3
Chemical PropertiesBack Directory
[Boiling point ]

574.4±60.0 °C(Predicted)
[density ]

1.57±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO:50.0(Max Conc. mg/mL);116.74(Max Conc. mM)
[form ]

Solid
[pka]

13.06±0.50(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor. IC50: In Vitro: Eltanexor 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:
[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. DOI:10.1158/1078-0432.CCR-16-1580
[2] Hing ZA et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Jun 21. DOI:10.1038/leu.2016.136
[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. DOI:10.1038/leu.2016.145
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