| Ọmụmụ in vitro | Bosutinib nwere nhọrọ dị elu maka Src karịa kinases ezinụlọ na-abụghị Src, yana IC50 nke 1.2 nM, ma na-egbochi mgbasa nke cell na-adabere na Src nke ọma, yana IC50 nke 100 nM. Bosutinib gbochiri nke ukwuu nke Bcr-Abl-positive leukemia cell ahịrị KU812, K562, na MEG-01 mana ọ bụghị Molt-4, HL-60, Ramos, na ahịrị sel leukemia ndị ọzọ, yana IC50 nke 5 nM, 20 nM, n'otu n'otu. , na 20 nM, dị irè karịa STI-571. Dị ka STI-571, Bosutinib na-arụ ọrụ na Abl-MLV na-agbanwe eriri ma nwee ọrụ na-abawanye na IC50 nke 90 nM. Na mkpokọta nke 50 nM, 10-25 nM, na 200 nM, n'otu n'otu, Bosutinib wepụrụ Bcr-Abl na STAT5 na sel CML na v-Abl tyrosine phosphorylation nke egosipụtara na eriri, nke a na-eme ka mgbochi nke phosphorylation nke Bcr-Abl na-agbada n'okpuru akara Ly /Hk. Ọ bụ ezie na ọ pụghị igbochi mmụba na ndụ nke mkpụrụ ndụ cancer ara, ọ nwere ike ibelata mmegharị na mbuso agha nke mkpụrụ ndụ ara ara, IC50 bụ 250 nM, ma melite njikọ intercellular na nhazi nke β-catenin. |
| Na vivo ọmụmụ | Bosutinib dị irè na ụmụ oke ịgba ọtọ na-ebu Src-transformed fiber xenografts na HT29 xenografts na dose nke 60 mg / kg kwa ụbọchị, yana ụkpụrụ T / C nke 18% na 30%, n'otu n'otu. Nlekọta ọnụ nke Bosutinib na ụmụ oke maka ụbọchị 5 gbochiri uto nke etuto K562 n'ụzọ dabere na dose. E kpochapụrụ nnukwu etuto ahụ na dose nke 100 mg / kg, ọgwụgwọ na dose nke 150 mg / kg wepụrụ etuto ahụ na-enweghị nsị. E jiri ya tụnyere mmetụta na tumor transplanted HT29, Bosutinib na dose nke 75 mg / kg, ugboro abụọ n'ụbọchị, nwere ike igbochi uto tumor na ụmụ oke na-ebu Colo205 transplanted tumor, ọ dịghị mmetụta dị elu mgbe ọ mụbara dose ahụ, ma 50 mg / kilogram dose enweghị mmetụta. |
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