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编 号:F194639
分子式:C32H37N5O6
分子量:587.67
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10mM*1mL in DMSO
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1mg
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5mg
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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.

体内研究:
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.Animal Model:Mouse xenograft model of SNU-16 human gastric cancer
Dosage:6.25 to 50 mg/kg
Administration:Orally, once daily for 14 days
Result:Inhibited tumor growth in a dose-dependent manner.

体外研究:
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.
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