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Eltanexor

Chemical Structure : Eltanexor

CAS No.: 1642300-52-4

Eltanexor (KPT-8602;KPT8602)

Catalog No.: PC-42150Not For Human Use, Lab Use Only.

Eltanexor (KPT-8602) is a second-generation SINE, orally bioavailable Exportin 1 (XPO1,CRM1) inhibitor with markedly reduced brain penetration compared to selinexor (30-fold less).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Eltanexor (KPT-8602) is a second-generation SINE, orally bioavailable Exportin 1 (XPO1,CRM1) inhibitor with markedly reduced brain penetration compared to selinexor (30-fold less).
Eltanexor (KPT-8602) inhibits viability of human AML cell lines in vitro with IC50 of 20−211 nM, more active than the first-generation XPO1 inhibitor, selinexor.
Eltanexor (KPT-8602) exhibits greater anti-leukemic efficacy against both leukemic blasts and LICs in AML patient-derived xenograft models, with no effect on normal hematopoietic stem and progenitor cell (HSPC) frequency.

Physicochemical Properties

M.Wt 428.2913
Formula C17H10F6N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 4.72 mg/mL

Chemical Name/SMILES

5-Pyrimidineacetamide, α-[[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]methylene]-, (αE)-

References

1. Etchin J, et al. Leukemia. 2017 Jan;31(1):143-150.

2. Hing ZA, et al. Leukemia. 2016 Dec;30(12):2364-2372.

3. Vercruysse T, et al. Clin Cancer Res. 2017 May 15;23(10):2528-2541.

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