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KPT-8602

Names

[ CAS No. ]:
1642300-52-4

[ Name ]:
KPT-8602

[Synonym ]:
eltanexor
5-Pyrimidineacetamide, α-[[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]methylene]-, (αE)-
(2E)-3-{3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}-2-(5-pyrimidinyl)acrylamide
KPT-8602

Biological Activity

[Description]:

KPT-8602 is a second-generation exportin-1 inhibitor, shows similar in vitro potency compared with KPT-330.In vitro: KPT-8602 induces caspase-dependent apoptosis in a panel of leukemic cell lines in vitro. Using CRISPR/Cas9 genome editing we demonstrats the specificity of KPT-8602 for cysteine 528 in the cargo-binding groove of XPO1 and validats the drug target interaction. [1]In vivo: KPT-8602 shows potent anti-leukemia activity in a mouse ALL model as well as in patient-derived T- and B-ALL xenograft models without affecting normal hematopoiesis.[1]

[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.


[Related Small Molecules]

KPT 330 | Eltanexor Z-isomer | KPT-185 | KPT-276 | Verdinexor

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
574.4±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H10F6N6O

[ Molecular Weight ]:
428.291

[ Flash Point ]:
301.2±32.9 °C

[ Exact Mass ]:
428.082031

[ LogP ]:
2.83

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.594

[ Storage condition ]:
-20℃

Related Compounds