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KPT-8602 (Z-isomer) manufacturers
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| | KPT-8602 (Z-isomer) Basic information |
| Product Name: | KPT-8602 (Z-isomer) | | Synonyms: | KPT-8602 (Z-isomer);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;Eltanexor Z-isomer;5-Pyrimidineacetamide, α-[[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]methylene]-, (αZ)-;Eltanexor Z isomer,Eltanexor Zisomer;(Z)-Eltanexor | | CAS: | 1642300-78-4 | | MF: | C17H10F6N6O | | MW: | 428.3 | | EINECS: | | | Product Categories: | | | Mol File: | 1642300-78-4.mol |  |
| | KPT-8602 (Z-isomer) Chemical Properties |
| 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) | | pka | 13.06±0.50(Predicted) | | form | Solid | | color | Light yellow to yellow |
| | KPT-8602 (Z-isomer) Usage And Synthesis |
| 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 |
| | KPT-8602 (Z-isomer) Preparation Products And Raw materials |
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