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Bosutinib (CAS# 380843-75-4) Chithunzi Chowonetsedwa
  • Bosutinib (CAS# 380843-75-4) 1

Bosutinib (CAS# 380843-75-4)

Chemical Property:

Molecular Formula C26H29Cl2N5O3
Molar Misa 530.45
Kuchulukana 1.36
Melting Point 116-120 ºC
Boling Point 649.7±55.0 °C(Zonenedweratu)
Pophulikira 346.7°C
Kusungunuka Zosungunuka mu DMSO, osati m'madzi
Kuthamanga kwa Vapor 0-0Pa pa 20 ℃
Maonekedwe Zolimba
Mtundu zoyera mpaka zofiirira
pKa 7.63±0.10 (Zonenedweratu)
Mkhalidwe Wosungira kutentha kwapanyumba
Kukhazikika Kukhazikika kwa zaka 2 kuyambira tsiku logula monga momwe zaperekedwa. Zothetsera mu DMSO zitha kusungidwa pa -20°C kwa mwezi umodzi.
Refractive Index 1.651
Maphunziro a in vitro Bosutinib ili ndi kusankha kwapamwamba kwa Src kuposa non-Src family kinases, ndi IC50 ya 1.2 nM, ndipo imalepheretsa kufalikira kwa maselo a Src, ndi IC50 ya 100 nM. Bosutinib idaletsa kwambiri kuchuluka kwa ma cell a Bcr-Abl-positive leukemia cell KU812, K562, ndi MEG-01 koma osati Molt-4, HL-60, Ramos, ndi ma cell ena a leukemia, okhala ndi IC50 ya 5 nM, 20 nM, motsatana. , ndi 20 nM, yothandiza kwambiri kuposa STI-571. Mofanana ndi STI-571, Bosutinib imagwira ntchito pazitsulo zosintha za Abl-MLV ndipo imakhala ndi ntchito yowonjezereka ndi IC50 ya 90 nM. Pazambiri za 50 nM, 10-25 nM, ndi 200 nM, motsatira, Bosutinib adachotsa Bcr-Abl ndi STAT5 m'maselo a CML ndi v-Abl tyrosine phosphorylation yowonetsedwa mu ulusi, izi zimapangitsa kuti phosphorylation ya Bcr-Abl ikhale pansi pamtsinje. /Hk. Ngakhale sizingalepheretse kuchulukana ndi kupulumuka kwa maselo a khansa ya m'mawere, zimatha kuchepetsa kwambiri kusuntha ndi kuwukira kwa ma cell a khansa ya m'mawere, IC50 ndi 250 nM, ndikuwongolera kulumikizana kwapakati ndi membrane kukhazikika kwa β-catenin.
Kuphunzira mu vivo Bosutinib inali yothandiza pa mbewa zamaliseche zokhala ndi Src-transformed fiber xenografts ndi HT29 xenografts pa mlingo wa 60 mg / kg patsiku, ndi T / C zamtengo wapatali za 18% ndi 30%, motero. Kuwongolera pakamwa kwa Bosutinib kwa mbewa kwa masiku 5 kunalepheretsa kwambiri kukula kwa zotupa za K562 motengera mlingo. Zotupa zazikulu zinathetsedwa pa mlingo wa 100 mg / kg, mankhwala pa mlingo wa 150 mg / kg anachotsa zotupa popanda poizoni. Poyerekeza ndi zotsatira za chotupa chopatsirana cha HT29, Bosutinib pa mlingo wa 75 mg/kg, kawiri pa tsiku, amatha kuletsa kukula kwa chotupa mu mbewa zamaliseche zokhala ndi chotupa cha Colo205, panalibe zotsatira zapamwamba pambuyo powonjezera mlingo, koma 50 mg/ kg mlingo unalibe mphamvu.

Tsatanetsatane wa Zamalonda

Zolemba Zamalonda

Zizindikiro Zowopsa Xi - Zosangalatsa
Zizindikiro Zowopsa 36 - Zokhumudwitsa m'maso
Kufotokozera Zachitetezo 26 - Mukakumana ndi maso, yambani nthawi yomweyo ndi madzi ambiri ndikupempha upangiri wamankhwala.
WGK Germany 3
HS kodi 29335990

 

Mawu Oyamba

Bosutinib ndi double inhibitor ya Src/Abl yokhala ndi IC50 ya 1.2 nM ndi 1 nM, motsatana.

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