Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
Purity: ≥98%
Formula Markup: C30H38N8O2
Formula Weight: 542.67544
CAS Number: 1913252-04-6
Notes: JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).{48431,48432} It inhibits colony formation of primary human CD34+ chronic myelogenous leukemia (CML) stem/progenitor cells but not non-cancerous human CD34+ hematopoietic stem/progenitor cells when used at concentrations ranging from 0.5 to 5 µM.{48432} It also reduces global levels of trimethylated histone 3 lysine 27 (H3K27Me3), a mark that is regulated by PRC2, in K562 cells. JQEZ5 (75 mg/kg per day) induces regression of tumors in an EZH2-driven transgenic mouse model of lung adenocarcinoma.{48431}
Deutsch
English
