1642300-52-4

1642300-52-4 structure

Name: KPT-8602
Chemical Name: eltanexor
CAS Number: 1642300-52-4
Molecular Formula: C₁₇H₁₀F₆N₆O
Molecular Weight: 428.291
Catalog: Signaling Pathways Membrane Transporter/Ion Channel CRM1
Create Date: 2018-03-15 08:00:00
Modify Date: 2024-01-09 18:48:08
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]

Name	eltanexor
Synonyms	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

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.