货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V57415-1ml	10mM in DMSO	￥9470.00 V57415-1ml ￥9470.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V57415-1ml

10mM in DMSO

￥9470.00

货期：3-5天

产品描述：

E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, 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. Overall, the in vitro and in vivo studies confirm that E7090 is a potent and selective FGFRs inhibitor, showing promising antitumor activities with wider therapeutic windows in preclinical cancer models harboring FGFRs gene abnormalities. 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 also inhibited the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nM.
E7090 succinate inhibited 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 succinate 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.

保存条件：

-80°C 12个月; -20°C 6个月, 干燥

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.307 ml	6.537 ml	13.075 ml
5 mM	0.261 ml	1.307 ml	2.615 ml
10 mM	0.131 ml	0.654 ml	1.307 ml
50 mM	0.026 ml	0.131 ml	0.261 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。

参考文献

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