| Barashada in vitro | Bosutinib wuxuu leeyahay xulashada sare ee Src marka loo eego non-Src kinase qoyska, oo leh IC50 ee 1.2 nM, oo si wax ku ool ah u joojiso kororka unugyada Src-ku-tiirsan, oo leh IC50 ee 100 nM. Bosutinib wuxuu si weyn u xakameeyey faafinta khadadka unugyada leukemia-ka ee Bcr-Abl-positive leukemia KU812, K562, iyo MEG-01 laakiin maaha Molt-4, HL-60, Ramos, iyo khadadka unugyada kale ee leukemia, oo leh IC50 ee 5 nM, 20 nM, siday u kala horreeyaan. , iyo 20 nM, oo ka waxtar badan STI-571. Si la mid ah STI-571, Bosutinib wuxuu ku shaqeeyaa Abl-MLV beddelka fiilooyinka wuxuuna leeyahay hawlo fican oo leh IC50 ee 90 nM. Marka la eego 50 nM, 10-25 nM, iyo 200 nM, siday u kala horreeyaan, Bosutinib waxa laga saaray Bcr-Abl iyo STAT5 ee unugyada CML iyo v-Abl tyrosine phosphorylation ee lagu muujiyay fiilooyinka, tani waxay keenaysaa in la joojiyo fosforyaalka Bcr-Abl ee hoos-u-dhaca calaamadaynta. /Hck. Inkasta oo aysan joojin karin faafinta iyo badbaadada unugyada kansarka naasaha, waxay si weyn u yareeyn kartaa dhaqdhaqaaqa iyo duulaanka unugyada kansarka naasaha, IC50 waa 250 nM, waxayna hagaajinaysaa adhesion intercellular iyo xuubka xuubka β-catenin. |
| In vivo waxbarasho | Bosutinib wuxuu wax ku ool u ahaa jiirarka qaawan ee Src-beddelay fiber xenografts iyo HT29 xenografts ee qiyaasta 60 mg / kg maalintii, oo leh qiimaha T / C ee 18% iyo 30%, siday u kala horreeyaan. Maamulka afka ee Bosutinib ee jiirarka 5 maalmood ayaa si weyn u joojiyay koritaanka burooyinka K562 qaab ku-tiirsanaan ah. Burooyinka waaweyn ayaa lagu ciribtiray qiyaasta 100 mg / kg, daaweynta qiyaasta 150 mg / kg burooyinka laga saaray iyada oo aan sun lahayn. Marka la barbardhigo saameynta HT29 ee buro la tallaalay, Bosutinib oo ah qiyaasta 75 mg / kg, laba jeer maalintii, waxay joojin kartaa koritaanka burooyinka jiirarka qaawan ee Colo205 ee buro la tallaalay, ma jirin saameyn sare ka dib kordhinta qiyaasta, laakiin 50 mg / qiyaasta kg wax saameyn ah kuma yeelan. |
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