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E7090 

目录号: HY-101466
产品使用指南

E7090 是一种有效的,具有口服活性的选择性 FGFR 抑制剂,对 FGFR1/FGFR2/FGFR3/FGFR4IC50 值分别为 0.71 nM、0.50 nM、1.2 nM 和120 nM。

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E7090 Chemical Structure

E7090 Chemical Structure

CAS No. : 1622204-21-0

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查看 FGFR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[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 inhibits the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nM[1].
E7090 inhibits 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 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].

MCE 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 hours
Result: Inhibited FGFR phosphorylation with an IC50 value of 1.2 nM.
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[1].
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2].

MCE 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

587.67

Formula

C32H37N5O6

CAS 号
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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
E7090
目录号:
HY-101466
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