CPDB0157 | BI-847325 | I-BI-847325 i-BEK / Aurora kinase inhibitor ekhethiweyo kunye ne-IC50 ixabiso le-3, i-25, i-15, i-25, kunye ne-4 nM ye-X. laevis Aurora B, i-Aurora A kunye ne-Aurora C, kunye ne-MEK1 yabantu kunye ne-MEK2, ngokulandelanayo. Inokuthintela ukukhula kunye nokusinda kwayo yomibini imigca yeseli ye-melanoma enganyangekiyo kunyango kunye neyeza, inciphisa ukubonakaliswa kwe-MEK kunye ne-Mcl-1 ngelixa inyusa ukubonakaliswa kweprotein ye-pro-apoptotic Bim. Kwi-70 mg / kg, i-BI-847325 yenza i-apoptosis kunyango-naive kunye neyeza-resistant xenografted melanoma in vivo. |