ASP5878 (3 mg/kg, orally, once daily) shows antitumor activity in a Hep3B2.1-7 subcutaneous xenograft and HCC orthotopic xenograft mouse model[1]. ASP5878 induces shrinkage of FGF19-expressing HCC xenograft model[1]. Animal Model: Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously)[1]. Dosage: 3 mg/kg. Administration: Orally once daily from days 14 to 52. Result: Induced tumor regression by 9% and 88% at 1 and 3 mg/kg, respectively, without affecting the body weight for 14 days. Induced the suppression of FGFR4 phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation. Animal Model: HCC orthotopic xenograft model (mouse)[1]. Dosage: 3 mg/kg. Administration: Orally once daily for 24 days. Result: Exhibited a lower tumor burden than vehicle- and sorafenibtreated mice. Induced sustained tumor regression without tumor regrowth.
In Vitro
ASP5878 shows potent antiproliferative activity in most human HCC cell lines[1]. ASP5878 inhibits FGFR4 phosphorylation in a concentration-dependent manner. ASP5878 treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation[1]. Cell Viability Assay[1] Cell Line: Human HCC cell lines. Concentration: 0-10000 nM. Incubation Time: 5 days. Result: HuH-7, Hep3B2.1-7, and JHH-7 cell lines exhibited potent sensitivity to ASP5878, with IC50 values of 27, 8.5, and 21 nmol/L, respectively. The growth inhibition rate of HLF was 64% and those of other ASP5878-sensitive cell lines were higher than 95% at 1000 nM.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Futami T, et al. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma. Mol Cancer Ther. 2017 Jan;16(1):68-75.
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