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ASP5878
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ASP5878图片
CAS NO:1453208-66-6
规格:98%
分子量:407.37
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
ASP5878是具有口服活性的、FGFR1、2、3、和4的抑制剂,其对FGFR1、2、3、和4激酶的IC50值分别为0.47nM、0.6nM、0.74nM和3.5nM。ASP5878具有潜在的抗肿瘤活性。
CAS:1453208-66-6
分子式:C18H19F2N5O4
分子量:407.37
纯度:98%
存储:Store at -20°C

Background:

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.