E7090 succinate

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

E7090 succinate 

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。

E7090 succinate

E7090 succinate Chemical Structure

CAS No. : 1879965-80-6

规格 价格 是否有货
5 mg ￥8500 询问价格 & 货期
10 mg ￥14500 询问价格 & 货期

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生物活性

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[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 IC50 value of 3 nM[1].
E7090 succinate inhibited SNU-16 cell proliferation with an IC50 value 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: SNU-16 cells.
Concentration: 0.4-100 nM.
Incubation Time: 4 h.
Result: Inhibited FGFR phosphorylation with an IC50 value 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.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

C36H43N5O10
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.
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.

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