| Mu bushakashatsi bwa vitro | Bosutinib ifite amahitamo menshi kuri Src kurusha kinase yumuryango utari Src, hamwe na IC50 ya 1.2 nM, kandi ikabuza neza ikwirakwizwa rya selile iterwa na Src, hamwe na IC50 ya 100 nM. Bosutinib yabujije cyane ikwirakwizwa rya Bcr-Abl-positif leukemia selile selile KU812, K562, na MEG-01 ariko ntabwo Molt-4, HL-60, Ramos, nindi mirongo ya selile ya leukemia, hamwe na IC50 ya 5 nM, 20 nM. , na 20 nM, ikora neza kuruta STI-571. Kimwe na STI-571, Bosutinib ikora kuri Abl-MLV ihindura fibre kandi ifite ibikorwa byinshi hamwe na IC50 ya 90 nM. Ubushuhe bwa 50 nM, 10-25 nM, na 200 nM, Bosutinib yacukuye Bcr-Abl na STAT5 mu tugari twa CML na v-Abl tyrosine fosifora yerekanwe muri fibre, ibi bivamo kubuza fosifora ya Bcr-Abl kumanuka yerekana Lyn. / Hck. Nubwo idashobora kubuza ikwirakwizwa rya kanseri yamabere no kubaho kwayo, irashobora kugabanya cyane kugenda no gutera ingirangingo za kanseri y'ibere, IC50 ni 250 nM, kandi igateza imbere ingirabuzimafatizo hamwe na membrane ya β-catenin. |
| Mu bushakashatsi bwa vivo | Bosutinib yagize akamaro mu mbeba zambaye ubusa zifite Src yahinduwe fibre xenografts na HT29 xenografts ku kigero cya 60 mg / kg kumunsi, hamwe na T / C bifite agaciro ka 18% na 30%. Gutanga umunwa wa Bosutinib kumbeba muminsi 5 byabujije cyane gukura kwikibyimba K562 muburyo buterwa na dose. Ibibyimba binini byahanaguwe ku gipimo cya mg / kg 100, kuvurwa ku kigero cya mg / kg 150 yakuyeho ibibyimba nta burozi. Ugereranije n'ingaruka kuri HT29 yatewe ikibyimba, Bosutinib ku kigero cya 75 mg / kg, kabiri ku munsi, gishobora kubuza ikibyimba imbeba zambaye ubusa zifite ibibyimba byatewe na Colo205, nta ngaruka nini zigeze nyuma yo kongera igipimo, ariko 50 mg / ikinini cya kg ntacyo cyagize. |
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