MEK

IKATI #	Igama Lomkhiqizo	Incazelo
Idatha ye-CPDB0157	BI-847325	I-BI-847325 iyi-dual inhibitor ye-MEK/Aurora kinase enamanani e-IC50 angu-3, 25, 15, 25, no-4 nM we-X. laevis Aurora B, i-Aurora A yomuntu kanye ne-Aurora C, kanye ne-MEK1 yomuntu kanye ne-MEK2 ngokulandelanayo. Ingavimbela ukukhula nokuphila kwayo yomibili imigqa yeseli ye-melanoma engalapheki futhi engazweli emuthini, yehlise ukusho kwe-MEK ne-Mcl-1 kuyilapho ikhulisa ukubonakaliswa kwe-pro-apoptotic protein Bim. Ku-70 mg/kg, i-BI-847325 idala i-apoptosis ku-melanoma ye-xenografted engazweli ekwelapheni futhi emelana nomuthi ku-vivo.