| 产品描述： | Fisogatinib (BLU-554)是一种有效的、高度选择性的、具有口服活性的FGFR4抑制剂，IC50为5 nM。对FGFR1-3的IC50范围为624-2203 nM |
| 靶点： |
FGFR4(Cell-free assay):5 nM;FGFR |
| 体外研究： |
BLU-554与FGFR4相互作用，对FGFR4的抑制具有高效力和选择性 |
| 体内研究： |
BLU-554在肿瘤模型中具有良好的耐受性。在肝癌模型中诱导肿瘤消退 |
| 细胞实验： |
Cell lines: ST8814 resistant cells Concentrations: 1 µM Incubation Time: 4 h Method: ST8814 resistant cells were treated with DMSO or BLU-554 at 1 µM for 4 hrs. |
| 动物实验： |
Animal Models: Male FVB/NRj mice Dosages: 10 mg/kg Administration: p.o. |
| 参考文献： |
1. Blueprint Medicines. BLU-554, A Novel, Potent and Selective Inhibitor ofFGFR4 for the Treatment of Liver Cancer. 50th th international liver congress. 2015. 2. Wang J, et al. Activation of Receptor Tyrosine Kinases Mediates Acquired Resistance to MEK Inhibition in Malignant Peripheral Nerve Sheath Tumors. Cancer Res. 2021 Feb 1;81(3):747-762. 3. Dogan-Topal B, et al. Quantification of FGFR4 inhibitor BLU-554 in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15;1110-1111:116-123. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.987 ml |
9.933 ml |
19.866 ml |
| 5 mM |
0.397 ml |
1.987 ml |
3.973 ml |
| 10 mM |
0.199 ml |
0.993 ml |
1.987 ml |
| 50 mM |
0.04 ml |
0.199 ml |
0.397 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京