ASP5878 inhibits the cell proliferation of HCC cell lines expressing FGF19. ASP5878 inhibits FGFR4 phosphorylation and its treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation in Hep3B2.1-7 cells.
In vivo
Oral administration of ASP5878 at 3 mg/kg induces sustained tumor regression in a subcutaneous xenograft mouse model using Hep3B2.1-7. In HuH-7, an orthotopic xenograft mouse model, ASP5878 induces complete tumor regression and dramatically extended the survival of the mice.
1.Kikuchi A, Suzuki T, Nakazawa T, Iizuka M, Nakayama A, Ozawa T, Kameda M, Shindoh N, Terasaka T, Hirano M et al.. (2017) ASP5878, a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance.. Cancer Sci, 108 (2):(236-242). [PMID:27885740][10.1021/op500134e]
2.Kuriwaki I, Kameda M, Iikubo K, Hisamichi H, Kawamoto Y, Kikuchi S, Moritomo H, Terasaka T, Iwai Y, Noda A et al.. (2022) Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity.. Bioorg Med Chem, 59 (13):(116657). [PMID:35219181][10.1021/op500134e]
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G2228315