| Thuto ea in vitro | Bosutinib e na le khetho e phahameng ea Src ho feta non-Src family kinases, e nang le IC50 ea 1.2 nM, 'me e thibela ka katleho ho ata ha lisele tse itšetlehileng ka Src, ka IC50 ea 100 nM. Bosutinib e thibetse haholo ho ata ha Bcr-Abl-positive leukemia cell lines KU812, K562, le MEG-01 empa eseng Molt-4, HL-60, Ramos, le lisele tse ling tsa leukemia, tse nang le IC50 ea 5 nM, 20 nM, ka ho latellana. , le 20 nM, e sebetsa ho feta STI-571. Ho tšoana le STI-571, Bosutinib e sebetsa ho Abl-MLV e fetolang likhoele 'me e na le ts'ebetso ea ho ata ka IC50 ea 90 nM. Libakeng tsa 50 nM, 10-25 nM, le 200 nM, ka ho latellana, Bosutinib e ntšitse Bcr-Abl le STAT5 liseleng tsa CML le v-Abl tyrosine phosphorylation e hlahisoang ka likhoele, sena se fella ka ho thibela phosphorylation ea Bcr-Abl e bontšang pontšo e tlase ea noka. /Hck. Le hoja e ke ke ea thibela ho ata le ho phela ha lisele tsa mofetše oa matsoele, e ka fokotsa haholo motsamao le tlhaselo ea lisele tsa mofetše oa matsoele, IC50 ke 250 nM, le ho ntlafatsa khokahano ea li-intercellular le membrane localization ea β-catenin. |
| Thuto ea in vivo | Bosutinib e ne e sebetsa hantle ho litoeba tse hlobotseng tse nang le Src-transformed fiber xenografts le HT29 xenografts ka tekanyo ea 60 mg / kg ka letsatsi, ka litekanyetso tsa T / C tsa 18% le 30%, ka ho latellana. Tsamaiso ea molomo ea Bosutinib ho litoeba bakeng sa matsatsi a 5 e ile ea thibela haholo kholo ea lihlahala tsa K562 ka mokhoa o itšetlehileng ka tekanyo. Lihlahala tse kholo li ile tsa felisoa ka tekanyo ea 100 mg / kg, phekolo ka tekanyo ea 150 mg / kg e tlosoa lihlahala tse se nang chefo. Ha ho bapisoa le phello ea hlahala e fetisitsoeng ea HT29, Bosutinib ka tekanyo ea 75 mg / kg, habeli ka letsatsi, e ka thibela kholo ea hlahala ho litoeba tse hlobotseng tse nang le hlahala e fetisitsoeng ea Colo205, ho ne ho se na phello e phahameng ka mor'a ho eketsa lethal dose, empa 50 mg / kg tekanyo e ne e se na phello. |
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