Sunitinib (CAS# 557795-19-4) Chithunzi Chowonetsedwa

Suntinib (CAS# 557795-19-4)

Chemical Property:

Molecular Formula	Chithunzi cha C22H27FN4O2
Misa ya Molar	398.47
Kuchulukana	1.2
Melting Point	189-191 ° C
Boling Point	572.1±50.0 °C(Zonenedweratu)
Pophulikira	299.8 ℃
Kusungunuka	25°C: DMSO
Kuthamanga kwa Vapor	3.13E-23mmHg pa 25°C
Maonekedwe	Crystalline ufa
Mtundu	Yellow mpaka Dark Orange
pKa	8.5 (pa 25 ℃)
Mkhalidwe Wosungira	2-8 ° C
MDL	Mtengo wa MFCD08273555
Maphunziro a in vitro	Sunitinib imagwira ntchito poletsa Kit ndi FLT-3. Sunitinib ndi ATP competitive inhibitor ya VEGFR2 (Flk1) ndi PDGFRβ, KI ndi 9 nM ndi 8 nM motero, kuchita pa VEGFR2 ndi PDGFR ndi yothandiza kwambiri kuposa FGFR-1, EGFR, Cdk2, Met,IGFR-1, Abl, ndi src zosankhidwa zinali zopitilira 10 kuposa. M'maselo a NIH-3T3 omwe ali ndi njala ya seramu akuwonetsa VEGFR2 kapena PDGFRβ, Sunitinib inhibited VEGF-dependent VEGFR2 phosphorylation ndi PDGF-dependent PDGFRβ phosphorylation ndi IC50 ya 10 nM ndi 10 nM, motero. Kwa maselo a NIH-3T3 owonjezera PDGFRβ kapena PDGFRα, Sunitinib inaletsa kufalikira komwe kunayambitsidwa ndi VEGF ndi IC50 ya 39 nM ndi 69 nM, motsatira. Sunitinib inhibited wild-type FLT3,FLT3-ITD, ndi FLT3-Asp835 phosphorylation ndi IC50 ya 250 nM, 50 nM, ndi 30 nM, motsatira. Sunitinib inaletsa kuchuluka kwa maselo a MV4; 11 ndi OC1-AML5 okhala ndi IC50 ya 8 nM ndi 14 nM, motero, ndipo anachititsa apoptosis m'njira yodalira mlingo.
Kuphunzira mu vivo	Mogwirizana ndi kuletsa kwakukulu, kosankha kwa phosphorylation ndi chizindikiro cha VEGFR2 kapena PDGFR mu vivo, Sunitinib (20-80 mg/kg/tsiku) yasonyezedwa kuti ndiyo imayambitsa mitundu yosiyanasiyana ya chotupa cha xenograft, kuphatikizapo HT-29, A431, Colo205, h. -460, SF763T,C6,A375, kapena MDA-MB-435 idawonetsa zochita zamphamvu kwambiri zodalira mlingo. Sunitinib pa mlingo wa 80 mg/kg/tsiku kwa masiku a 21 inachititsa kuti chotupa chiwonongeke mu 6 ya mbewa za 8, ndipo pamapeto a mankhwala, zotupa sizinayambikenso pa nthawi ya 110. Njira yachiwiri ya chithandizo ndi Sunitinib idakali yothandiza polimbana ndi zotupa, koma sanachire bwino pamzere woyamba wamankhwala. Chithandizo cha Sunitinib chinapangitsa kuchepa kwakukulu kwa chotupa cha MVD, chomwe chinachepetsedwa ndi ~ 40% mu SF763T gliomas. Chithandizo cha SU11248 chinapangitsa kuletsa kwathunthu kwa chotupa chowonjezereka cha luciferase-kufotokoza PC-3M xenografts, ngakhale kuti palibe kuchepa kwa kukula kwa chotupa. Mu chitsanzo cha FLT3-ITD chopangira mafupa, chithandizo cha Sunitinib (20 mg / kg / tsiku) chinalepheretsa kwambiri kukula kwa subcutaneous MV4; 11 (FLT3-ITD) xenografts ndi kukhala ndi moyo wautali.