ASP5878 |
| Catalog No.GC34476 |
ASP5878은 FGFR 1, 2, 3 및 4 키나제 활성에 대한 IC50 값이 0.47 nM, 0.6 nM, 0.74 nM 및 3.5 nM인 FGFR 1, 2, 3 및 4의 경구 활성 억제제입니다. ASP5878은 잠재적인 항종양 활성이 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1453208-66-6
Sample solution is provided at 25 µL, 10mM.
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ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity[1]. FGFR1|0.47 nM (IC50)|FGFR2|0.6 nM (IC50)|FGFR3|0.74 nM (IC50)|FGFR4|3.5 nM (IC50)
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.
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].
[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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