| Kev tshawb nrhiav hauv vitro | Bosutinib muaj kev xaiv ntau dua rau Src dua li cov tsis yog-Src tsev neeg kinases, nrog rau IC50 ntawm 1.2 nM, thiab zoo inhibits Src-dependent cell proliferation, nrog IC50 ntawm 100 nM. Bosutinib cuam tshuam qhov kev loj hlob ntawm Bcr-Abl-positive leukemia cell kab KU812, K562, thiab MEG-01 tab sis tsis yog Molt-4, HL-60, Ramos, thiab lwm yam kab mob leukemia, nrog IC50 ntawm 5 nM, 20 nM, feem. , thiab 20 nM, zoo dua STI-571. Zoo ib yam li STI-571, Bosutinib ua rau Abl-MLV hloov pauv fibers thiab muaj kev ua haujlwm loj hlob nrog IC50 ntawm 90 nM. Ntawm qhov siab ntawm 50 nM, 10-25 nM, thiab 200 nM, raws li, Bosutinib excised Bcr-Abl thiab STAT5 hauv CML hlwb thiab v-Abl tyrosine phosphorylation qhia hauv fibers, qhov no ua rau inhibition ntawm phosphorylation ntawm Bcr-Abl downstreaming signaling. /Hck. Txawm hais tias nws tsis tuaj yeem cuam tshuam qhov kev loj hlob thiab kev ciaj sia ntawm cov qog nqaij hlav cancer mis, nws tuaj yeem txo qis kev txav mus los thiab cuam tshuam ntawm cov qog nqaij hlav cancer mis, IC50 yog 250 nM, thiab txhim kho cov kev sib txuas ntawm cov hlwb thiab cov membrane localization ntawm β-catenin. |
| Hauv vivo kawm | Bosutinib tau txais txiaj ntsig zoo hauv cov nas liab liab uas muaj Src-hloov fiber ntau xenografts thiab HT29 xenografts ntawm ib koob ntawm 60 mg / kg ib hnub, nrog T / C qhov tseem ceeb ntawm 18% thiab 30%, feem. Kev tswj hwm qhov ncauj ntawm Bosutinib rau cov nas rau 5 hnub cuam tshuam qhov kev loj hlob ntawm K562 cov qog nyob rau hauv koob tshuaj. Cov qog loj tau tshem tawm ntawm qhov koob tshuaj ntawm 100 mg / kg, kev kho mob ntawm koob tshuaj 150 mg / kg tshem tawm cov qog uas tsis muaj tshuaj lom. Piv nrog rau cov nyhuv ntawm HT29 transplanted qog, Bosutinib ntawm ib koob ntawm 75 mg / kg, ob zaug ib hnub twg, tuaj yeem cuam tshuam cov qog loj hlob hauv cov nas liab liab bearing Colo205 transplanted qog, tsis muaj kev cuam tshuam ntau dua tom qab nce koob, tab sis 50 mg / kg koob tsis muaj txiaj ntsig. |
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