2102672-22-8

DK419 is a potent inhibitor of Wnt/β-catenin signaling and colorectal cancer growth. DK419 inhibited Wnt/β-catenin signaling, altered cellular oxygen consumption rate and induced production of pAMPK. DK419 inhibited the growth of CRC tumor cells in vitro, had good plasma exposure when dosed orally, and inhibited the growth of patient derived CRC240 tumor explants in mice dosed orally.

DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK[1].

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[1] Wang J, et al. Identification of DK419, a potent inhibitor of Wnt/β-catenin signaling and colorectal cancer growth. Bioorg Med Chem. 2018 Nov 1;26(20):5435-5442. DOI:10.1016/j.bmc.2018.09.016