CAS 1642300-52-4|KPT-8602

Introduction:Basic information about CAS 1642300-52-4|KPT-8602, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameKPT-8602
CAS Number1642300-52-4Molecular Weight428.291
Density1.6±0.1 g/cm3Boiling Point574.4±60.0 °C at 760 mmHg
Molecular FormulaC17H10F6N6OMelting Point/
MSDS/Flash Point301.2±32.9 °C

Names

Nameeltanexor
SynonymMore Synonyms

KPT-8602 BiologicalActivity

DescriptionKPT-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 CatalogSignaling Pathways >>Membrane Transporter/Ion Channel >>CRM1Research 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.

Chemical & Physical Properties

Density1.6±0.1 g/cm3
Boiling Point574.4±60.0 °C at 760 mmHg
Molecular FormulaC17H10F6N6O
Molecular Weight428.291
Flash Point301.2±32.9 °C
Exact Mass428.082031
LogP2.83
Vapour Pressure0.0±1.6 mmHg at 25°C
Index of Refraction1.594
Storage condition-20℃

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
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