ASP-5878

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ASP5878 有效抑制重组 FGFR1、2、3 和 4 的酪氨酸激酶活性，IC50 值为 0.47、0.60、0.74 和 3.5 nmol/L。

ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1 2 3 and 4 with IC50 values of 0.47 0.60 0.74 and 3.5 nmol/L.

Cell Viability Assay Cell Line:Human HCC cell lines.Concentration:0-1000 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.

Animal Model:Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously).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).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.

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Angiogenesis

FGFR

FGFR1/2/3/4

Cancer

Solid tumours

1453208-66-6

407.38

C18H19F2N5O4

>98% (HPLC)

DMSO:250 mg/mL?(613.69 mM)

COc1cc(OC)c(F)c(COc2cnc(Nc3cnn(CCO)c3)nc2)c1F

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(-20℃)

With Ice Pack

≥ 2 years