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