| Identification | Back 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 Properties | Back 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 Information | Back 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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