| Nazarin in vitro | Bosutinib yana da zaɓi mafi girma don Src fiye da kinases na dangin Src ba, tare da IC50 na 1.2 nM, kuma yana hana yaduwar kwayar halitta mai dogaro da Src, tare da IC50 na 100 nM. Bosutinib ya hana yaduwar kwayar cutar sankarar bargo ta Bcr-Abl-positive leukemia KU812, K562, da MEG-01 amma ba Molt-4, HL-60, Ramos, da sauran layin kwayar cutar sankarar bargo, tare da IC50 na 5 nM, 20 nM, bi da bi. , da 20 nM, mafi inganci fiye da STI-571. Kamar STI-571, Bosutinib yana aiki akan Abl-MLV yana canza zaruruwa kuma yana da aikin haɓaka tare da IC50 na 90 nM. A matakan 50 nM, 10-25 nM, da 200 nM, bi da bi, Bosutinib ya cire Bcr-Abl da STAT5 a cikin ƙwayoyin CML da v-Abl tyrosine phosphorylation da aka bayyana a cikin fibers, wannan yana haifar da hanawa na phosphorylation na Bcr-Abl downstreaming sigina. /Hk. Ko da yake ba zai iya hana yaduwa da rayuwa na nono ciwon daji Kwayoyin, zai iya muhimmanci rage motsi da mamayewa na nono Kwayoyin, IC50 ne 250 nM, da kuma inganta intercellular adhesion da membrane localization na β-catenin. |
| A cikin nazarin vivo | Bosutinib yana da tasiri a cikin tsirara mice masu ɗauke da Src-canzawar fiber xenografts da HT29 xenografts a kashi na 60 mg / kg kowace rana, tare da ƙimar T / C na 18% da 30%, bi da bi. Gudanar da baka na Bosutinib zuwa mice na tsawon kwanaki 5 yana hana haɓakar ciwace-ciwacen K562 ta hanyar dogaro da kashi. An kawar da manyan ciwace-ciwacen daji a kashi na 100 mg / kg, jiyya a kashi na 150 mg / kg cire ciwace-ciwacen ƙwayoyi ba tare da guba ba. Idan aka kwatanta da sakamako akan ƙwayar cutar da aka dasa HT29, Bosutinib a kashi na 75 mg / kg, sau biyu a rana, zai iya hana ci gaban ciwace-ciwacen ƙwayar cuta a cikin berayen tsirara waɗanda ke ɗauke da ƙwayar ƙwayar cuta ta Colo205, babu wani sakamako mafi girma bayan ƙara yawan adadin, amma 50 mg / kg kashi bai yi tasiri ba. |
![4-[(2-Furanmethyl)thio] -2-pentanone (4-Furfurylthio-2-pentanone) (CAS#180031-78-1)](https://cdn.globalso.com/xinchem/4-2-Furanmethyl-thio-2-pentanone -4-Furfurylthio-2-pentanone.png)
