E7090
目录号: PL01226 纯度: ≥99%
CAS No. :1622204-21-0
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中文名称
E7090
英文名称
E7090
英文别名
E7090;TN7CUD1NGA;5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamido)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide;5-[2-[[4-[1-(2-hydroxyethyl)piperidin-4-yl]benzoyl]amino]pyridin-4-yl]oxy-6-(2-methoxyethoxy)-N-methylindole-1-carboxamide;tasurgratinib;GTPL11414;BDBM142256;Fgf/fgfr pathway inhibitor E7090;BCP29727;NSC806388;SB18854;Example 22 [WO2014129477A1];E 7090; E7090;US8933099, 22;E-7090
Cas No.
1622204-21-0
分子式
C32H37N5O6
分子量
587.67
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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/FGFR4 的 IC50 值分别为 0.71 nM、0.50 nM、1.2 nM 和120 nM。
生物活性
E7090 is an orally available, potent, and selective FGFR inhibitor with IC 50 s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.
性状
Solid
IC50 & Target[1][2]
FGFR1 0.71 nM (IC50) FGFR2 0.50 nM (IC
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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.
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.
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (170.16 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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