AZ 13824374 New
Chemical Name: (1R,2R,5S)-11-(8-((1-(2-Fluoro-2-methylpropyl)piperidin-4-yl)amino)-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl)-2-isopropyl-2,3,5,6-tetrahydro-1,5-epiminobenzo[d]azocin-4(1H)-one
Biological ActivityAZ 13824374 is a potent and selective inhibitor of ATPase family AAA domain-containing protein 2 (ATAD2) bromodomain (pIC50 values are 6.2 and 8.2 in NanoBRET assay and FRET assay, respectively). It is >100-fold selective over a range of epigenetic targets from ROMOscan panel (DiscoveRx Corp.). AZ 13824374 shows cellular target engagement (cellular inhibition pIC50 = 6.9) and antiproliferative activity in a range of breast cancer cell lines.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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