| Description | ASP5878isanovelFGFR-selectiveinhibitorwithIC50valuesof0.47,0.60,0.74,and3.5nmol/LforrecombinantFGFR1,2,3,and4,respectively. | ||||||||
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| Targets |
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| Invitro | ASP5878inhibitsthecellproliferationofHCCcelllinesexpressingFGF19.ASP5878inhibitsFGFR4phosphorylationanditstreatmentresultsinthesuppressionofphosphorylation,mobilityshiftofFRS2,andsuppressionofERKphosphorylationinHep3B2.1-7cells[1]. | ||||||||
| Invivo | OraladmiNISTrationofASP5878at3mg/kginducessustainedtumorregressioninasubcutaneousxenograftmousemodelusingHep3B2.1-7.InHuH-7,anorthotopicxenograftmousemodel,ASP5878inducescompletetumorregressionanddramaticallyextendedthesurvivalofthemice[1]. |
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