CH5183284 (Zoligratinib, Debio1347) is a potent, selective and orally available FGFR1/2/3 inhibitor with enzyme IC50 of 9.3/7.6/22 nM, respectively.
CH-5183284 displays >10-fold selectivity over FGFR4, and >100-fold over KDR, Src, and other kinases.
CH-5183284 displays preferential antitumor activity against cancer cells with various FGFR genetic alterations in a panel of 327 cancer cell lines and in xenograft models.
CH-5183284 can inhibit FGFR2 harboring one type of the gatekeeper mutation and blocks FGFR2 V564F-driven tumor growth.
