| 产品描述: | Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. |
| 靶点: |
FGFR1;FGFR2;FGFR3;FGFR4 |
| 体外研究: |
Of the 24 cell lines, 2 FGFR1-amplified lung cancer (LC) cell lines, H1581 and DMS114, show extreme sensitivity to Rogaratinib (BAY1163877) (GI50 values ranging from 36 to 244 nM). Treatment with Rogaratinib results in a significant decrease in colonies formed by H1581P cells, but not by H1581AR and BR cells. Ectopic expression of Met significantly induces resistance to Rogaratinib in MTT assays. Met overexpression induces activation of downstream extracellular signal-regulated kinase 1/2 (ERK1/2) and AKT, which cannot be abrogated by Rogaratinib treatment. |
| 参考文献: |
1. Kim SM, et al. Activation of the Met kinase confers acquired drug resistance in FGFR-targeted lung cancer therapy. Oncogenesis. 2016 Jul 18;5(7):e241. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.143 ml |
10.717 ml |
21.433 ml |
| 5 mM |
0.429 ml |
2.143 ml |
4.287 ml |
| 10 mM |
0.214 ml |
1.072 ml |
2.143 ml |
| 50 mM |
0.043 ml |
0.214 ml |
0.429 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。 |