| In vitro kudzidza | Bosutinib ine yakakwira selectivity yeSrc pane isiri-Src family kinases, ine IC50 ye1.2 nM, uye zvinobudirira inhibits Src-inotsamira cell kuwanda, ine IC50 ye100 nM. Bosutinib yakadzivisa zvakanyanya kuwanda kweBcr-Abl-positive leukemia cell lines KU812, K562, uye MEG-01 asi kwete Molt-4, HL-60, Ramos, uye mamwe masero eukemia, ane IC50 ye5 nM, 20 nM, zvichiteerana. , uye 20 nM, inoshanda kupfuura STI-571. Zvakafanana neSTI-571, Bosutinib inoshanda paAbl-MLV inoshandura fiber uye ine basa rinowedzera neIC50 ye90 nM. Pakuiswa kwe50 nM, 10-25 nM, uye 200 nM, zvichiteerana, Bosutinib yakabvisa Bcr-Abl uye STAT5 mumasero eCML uye v-Abl tyrosine phosphorylation inoratidzwa mumafibers, izvi zvinoguma nekudzivirirwa kwephosphorylation yeBcr-Abl inoratidzira pasi pemvura. /Hck. Kunyange zvazvo isingakwanisi kudzivisa kuwedzera uye kupona kwemasero emukenza wezamu, inogona kuderedza zvakanyanya kufamba uye kupinda kwemasero emukenza wezamu, IC50 ndeye 250 nM, uye inovandudza intercellular adhesion uye membrane localization ye β-catenin. |
| In vivo kudzidza | Bosutinib yakashanda mu nude mice inotakura Src-transformed fiber xenografts uye HT29 xenografts pamutengo we 60 mg / kg pazuva, neT / C inokosha ye18% uye 30%, maererano. Oral administration yeBosutinib kune mbeva kwemazuva 5 zvakanyanya kuvharidzira kukura kweK562 tumors nenzira inoenderana nedosi. Zvirwere zvakakura zvakapedzwa pachiyero che 100 mg / kg, kurapwa pamwero we 150 mg / kg yakabviswa mapundu asina chepfu. Zvichienzaniswa nemhedzisiro yeHT29 yakasimwa bundu, Bosutinib pachiyero che 75 mg/kg, kaviri pazuva, inogona kutadzisa bundu kukura mumakonzo asina kupfeka ane Colo205 akaisirwa bundu, pakanga pasina mhedzisiro yepamusoro mushure mekuwedzera dosi, asi iyo 50 mg/ kg dose yanga isingaite. |
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