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Sunitinib (CAS# 557795-19-4) Sawirka la soo bandhigay
  • Sunitinib (CAS# 557795-19-4) 1

Sunitinib (CAS# 557795-19-4)

Hantida Kiimikada:

Qaanuunka molecular C22H27FN4O2
Molar Mass 398.47
Cufnaanta 1.2
Meesha dhalaalaysa 189-191°C
Boling Point 572.1± 50.0 °C (La saadaaliyay)
Barta Fiishka 299.8 ℃
Solubility 25°C: DMSO
Uumiga Uumiga 3.13E-23mmHg at 25°C
Muuqashada Budada crystalline
Midabka Jaalle ilaa Liin madaw
pKa 8.5 ( saacada 25 ℃)
Xaalada Kaydinta 2-8°C
MDL MFCD08273555
Barashada in vitro Sunitinib waxay wax ku ool u tahay joojinta Kit iyo FLT-3. Sunitinib waa horjooge wax ku ool ah ATP tartanka VEGFR2 (Flk1) iyo PDGFRβ, KI waa 9 nM iyo 8 nM siday u kala horreeyaan, ku-dhaqanka VEGFR2 iyo PDGFR ayaa ka waxtar badan FGFR-1,EGFR,Cdk2,Met,IGFR-1,Abl,iyo xulashada src waxay ka badnaayeen 10 jeer. Unugyada NIH-3T3 ee serum-gaajaysan oo muujinaya VEGFR2 ama PDGFRβ, Sunitinib waxay joojiyeen VEGF-ku-tiirsanaanta VEGFR2 fosforyaalka iyo PDGF-ku-tiirsanaanta PDGFRβ fosforyaal leh IC50 ee 10 nM iyo 10 nM, siday u kala horreeyaan. Unugyada NIH-3T3 ee si xad dhaaf ah u muujinaya PDGFRβ ama PDGFRa, Sunitinib waxay joojisay fidinta ay keentay VEGF oo leh IC50 ee 39 nM iyo 69 nM, siday u kala horreeyaan. Sunitinib wuxuu joojiyay nooca duurjoogta ah ee FLT3,FLT3-ITD, iyo FLT3-Asp835 fosforyaalka leh IC50 ee 250 nM,50 nM, iyo 30 nM, siday u kala horreeyaan. Sunitinib waxay joojisay faafitaanka unugyada MV4;11 iyo OC1-AML5 ee leh IC50 ee 8 nM iyo 14 nM, siday u kala horreeyaan, iyo apoptosis-ka keentay hab ku-tiirsanaan ah.
In vivo waxbarasho Iyada oo la raacayo xannibaad la taaban karo oo la xushay ee fosforyaalka iyo calaamadaynta VEGFR2 ama PDGFR gudaha vivo, Sunitinib (20-80 mg/kg/maalintii) ayaa la muujiyay inuu mas'uul ka yahay noocyo kala duwan oo burooyinka xenograft, oo ay ku jiraan HT-29, A431, Colo205, h -460, SF763T,C6,A375, ama MDA-MB-435 waxay soo bandhigtay firfircoonida ka hortagga tumor-ku-tiirsanaanta si ballaaran. Sunitinib oo ah qiyaasta 80 mg/kg/maalintii 21 maalmood waxay keentay buro dib udhac ah oo dhamaystiran 6 ee jiirarka 8, iyo dhamaadka daaweynta, burooyinka dib uma soo kicin inta lagu jiro mudada 110-maalin ee kormeerka. Wareegii labaad ee daaweynta Sunitinib ayaa weli waxtar u leh ka hortagga burooyinka, laakiin si buuxda ugama soo kaban wareegii koowaad ee daaweynta. Daaweynta Sunitinib waxay keentay hoos u dhac weyn oo ku yimid buro MVD, taas oo la dhimay ~ 40% gliomas SF763T. Daaweynta SU11248 waxay keentay in si buuxda loo joojiyo koritaanka burooyinka dheeraadka ah ee luciferase-muujinta PC-3M xenografts, inkastoo aysan jirin hoos u dhac ku yimid cabbirka buro. Qaabka FLT3-ITD ee dhuuxa lafta ku-tallaalidda, daawaynta Sunitinib (20 mg/kg/maalintii) waxay si weyn u joojisay koritaanka MV4;11 (FLT3-ITD) xenografts iyo badbaadada dheeraadka ah.

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Sharaxaada Badbaadada 24/25 - Ka fogow taabashada maqaarka iyo indhaha.
Koodhka HS 29337900

 

Hordhac

Sunitinib waa horjoogeyaal badan oo la beegsanayo RTK oo lagu beegsanayo VEGFR2 (Flk-1) iyo PDGFRβ leh IC50 ee 80 nM iyo 2 nM, iyo sidoo kale xannibaya c-Kit.

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