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PLX8394 is a potent and selective inhibitor of B-RafV600E (IC50~5 nM).
IC50 value: ~5 nM
in vitro: PLX8394 potently inhibits phosphorylation of ERK1/2 in PRT #3 and PRT #4 cells in addition to parental cells. PLX8394 potently inhibits ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX8394 effectively reducs cyclin D3 and cyclin D1, phosphorylation of retinoblastoma protein, and expression of cyclin A2 in parental cells. PLX8394 reduces levels of these cell cycle markers in PRT #3 and PRT #4 cells. Consistent with these effects, PLX8394 inhibits EdU incorporation into PRT #3 and PRT #4 cells in S phase entry assays. PLX8394 inhibits ERK1/2 phosphorylation and the growth of vemurafenib-resistant cells harboring either a BRAF V600K/L505H double mutation or an transposon-induced, N-terminal truncated form of BRAF
|PLX8394 Basic information|
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