| Isifundo se-in vitro | I-Bosutinib ine-selectivity ephezulu ye-Src kune-non-Src family kinases, ene-IC50 ye-1.2 nM, kwaye inqanda ngokufanelekileyo i-Src-dependent cell proliferation, kunye ne-IC50 ye-100 nM. I-Bosutinib inqande kakhulu ukwanda kwe-Bcr-Abl-positive leukemia cell lines KU812, K562, kunye ne-MEG-01 kodwa kungekhona i-Molt-4, i-HL-60, i-Ramos, kunye nezinye iiseli ze-leukemia, kunye ne-IC50 ye-5 nM, i-20 nM, ngokulandelanayo. , kunye ne-20 nM, isebenza ngakumbi kune-STI-571. Ngokufana ne-STI-571, i-Bosutinib isebenza kwi-Abl-MLV yokuguqula iifayili kwaye inomsebenzi okhulayo kunye ne-IC50 ye-90 nM. Kugxininiso lwe-50 nM, i-10-25 nM, kunye ne-200 nM, ngokulandelanayo, i-Bosutinib ikhuphe i-Bcr-Abl kunye ne-STAT5 kwiiseli ze-CML kunye ne-v-Abl tyrosine phosphorylation echazwe kwiifibers, oku kubangela ukuvinjelwa kwe-phosphorylation ye-Bcr-Abn ezantsi komlambo. /Hck. Nangona ingenako ukuthintela ukwanda kunye nokusinda kweeseli zomhlaza webele, kunokunciphisa kakhulu ukuhamba kunye nokuhlasela kwamaseli omhlaza webele, i-IC50 yi-250 nM, kwaye iphucule i-intercellular adhesion kunye ne-membrane yendawo ye-β-catenin. |
| Kwisifundo se-vivo | I-Bosutinib yayisebenza kwiigundane ezinqunu ezithwele i-fiber xenografts ye-Src-transformed kunye ne-HT29 xenografts kwi-dose ye-60 mg / kg ngosuku, kunye nexabiso le-T / C le-18% kunye ne-30%, ngokulandelanayo. Ukulawulwa komlomo we-Bosutinib kwiigundane kwiintsuku ze-5 kuthintele kakhulu ukukhula kwe-K562 tumors ngendlela exhomekeke kwidosi. Amathumba amakhulu apheliswa kwi-dose ye-100 mg / kg, unyango kwi-dose ye-150 mg / kg isuswe izicubu ezingenayo ubuthi. Xa kuthelekiswa nesiphumo kwi-HT29 yokufakelwa kwe-tumor, i-Bosutinib kwi-dose ye-75 mg / kg, kabini ngosuku, inokuthintela ukukhula kwe-tumor kwiigundane ezingenanto ezithwele i-Colo205 i-tumor efakwe kwi-tumor, kwakungekho siphumo esiphezulu emva kokunyusa umthamo, kodwa i-50 mg / I-kg idosi ayizange ibe nefuthe. |
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