| CAS NO: | 1453208-66-6 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 1453208-66-6 |
| Canonical SMILES | OCCN1N=CC(NC2=NC=C(OCC3=C(F)C(OC)=CC(OC)=C3F)C=N2)=C1 |
| 分子式 | C18H19F2N5O4 |
| 分子量 | 407.37 |
| 溶解度 | DMSO : ≥ 250 mg/mL (613.69 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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