| 产品描述: | E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively. |
| 靶点: |
FGFR1:0.71 nM (IC50); FGFR2:0.50 nM (IC50); FGFR3:1.2 nM (IC50); FGFR4:120 nM (IC50) |
| 体外研究: |
Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner[1]. E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2]. |
| 体内研究: |
E7090 inhibits the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nM. E7090 inhibits SNU-16 cell proliferation with an IC50 value of 5.7 nM. E7090 inhibits proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling. E7090 has interaction kinetics with FGFR1 kinases intermediate between those of the two representative inhibitors, and the residence time of E7090 succinate is 19 minutes. |
| 参考文献: |
1. Saori Watanabe Miyano, et al. E7090: A potent and selective FGFR inhibitor with activity in multiple FGFR-driven cancer models with distinct mechanisms of activation. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA. 2. Saori Watanabe Miyano, et al. E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models. Mol Cancer Ther. 2016 Nov;15(11):2630-2639. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.702 ml |
8.508 ml |
17.016 ml |
| 5 mM |
0.34 ml |
1.702 ml |
3.403 ml |
| 10 mM |
0.17 ml |
0.851 ml |
1.702 ml |
| 50 mM |
0.034 ml |
0.17 ml |
0.34 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。 |