Cas No.: | 1642300-52-4 |
Chemical Name: | 5-Pyrimidineacetamide, α-[[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]methylene]-, (αE)- |
Synonyms: | KPT-8602;KPT8602 |
SMILES: | FC(C1C=C(C2N=CN(C=C(C(=O)N)C3C=NC=NC=3)N=2)C=C(C(F)(F)F)C=1)(F)F |
Formula: | C17H10F6N6O |
M.Wt: | 428.2913 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A second-generation SINE, orally bioavailable Exportin 1 (XPO1,CRM1) inhibitor with markedly reduced brain penetration compared to selinexor (30-fold less); inhibits viability of human AML cell lines in vitro with IC50 of 20−211 nM, more active than the first-generation XPO1 inhibitor, selinexor; 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.Blood CancerPhase 2 Clinical |