您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > E7090 succinate
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
E7090 succinate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
E7090 succinate图片
CAS NO:1879965-80-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
E7090 succinate 是具有口服活性的、选择性的、有效的FGFR1/2/3抑制剂,其对 FGFR1/2/3/4 的IC50值分别为 0.71 nM、0.50 nM、1.2 nM 和120 nM。
生物活性

E7090 succinate is an orally available, selective and potent inhibitor ofFGFR1,FGFR2andFGFR3tyrosine kinase activities, withIC50values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively[1].

IC50& Target[2]

FGFR1

0.71 nM (IC50)

FGFR2

0.50 nM (IC50)

FGFR3

1.2 nM (IC50)

FGFR4

120 nM (IC50)

体外研究
(In Vitro)

E7090 also inhibited the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50value of 3 nM[1].
E7090 succinate inhibited SNU-16 cell proliferation with an IC50value of 5.7 nM[2].
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[1].
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[1].

Western Blot Analysis[1]

Cell Line:SNU-16 cells.
Concentration:0.4-100 nM.
Incubation Time:4 h.
Result:Inhibited FGFR phosphorylation with an IC50value of 1.2 nmol/L. Inhibited the phosphorylation of FRS2a, ERK1/2, and AKT, molecules downstream of FGFRs, in a dose-dependent manner.
体内研究
(In Vivo)

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[1]. E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2.

Animal Model:Mouse xenograft model of SNU-16 human gastric cancer[2].
Dosage:6.25 to 50 mg/kg.
Administration:Orally, once daily for 14 days.
Result:Inhibited tumor growth in a dose-dependent manner.
Clinical Trial
分子量

764.82

Formula

C32H37N5O6.3/2C4H6O4

CAS 号

1879965-80-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.