Sharaxaada

Ribociclib (LEE01) waa CDK4/6 horjooge aad u gaar ah oo leh IC50 qiyamka 10 nM iyo 39 nM, siday u kala horreeyaan, waxayna in ka badan 1,000-laab ka awood yar tahay isku-xidhka cyclin B/CDK1.

In Vitro

Daweynta koox ka kooban 17 khadadka unugyada neuroblastoma oo leh Ribociclib (LEE011) oo u dhexeeya qiyaas afar-log ah (10 ilaa 10,000 nM). Daawaynta Ribociclib waxay si weyn u joojisaa korriinka substrate-ka ee ku xiran kantaroolka 12 ee 17ka xariiqda unugyada neuroblastoma ee la baaray (macnaha IC50=306±68 nM, iyadoo la tixgelinayo khadadka xasaasiga ah oo keliya, halkaasoo dareenka lagu qeexay IC50 oo ka yar 1μDaaweynta M. Ribociclib ee labada xariiq ee unugyada neuroblastoma (BE2C iyo IMR5) oo leh dareenka la muujiyay ee CDK4 / 6 xannibaadda waxay keenaysaa qiyaasta qiyaasta unugyada unugyada wareega G0 / G1 ee wareegga unugyada. Xarigan G0/G1 waxa uu noqonayaa mid muhiim ah marka la eego xadiga Ribociclib ee 100 nM (p=0.007) iyo 250 nM (p=0.01), siday u kala horreeyaan.

Jiirarka difaaca jirka ee CB17 ee sita BE2C, NB-1643 (MYCN la kordhiyey, xasaasiga ah in vitro), ama EBC1 (aan la kordhin, adkaysi u leh in vitro) xenografts ayaa lagu daaweeyaa hal mar maalintii 21 maalmood oo leh Ribociclib (LEE011; 200 mg/kg) ama xakamaynta baabuurta. Istaraatiijiyadan qiyaasta si fiican ayaa loo dulqaatay, maadaama aan miisaan lumis ama calaamado kale oo sun ah lagu arkay mid ka mid ah noocyada xenograft. Kobaca burada si weyn ayaa loo daahiyay 21ka maalmood ee daawaynta ee jiirarka ee BE2C ama 1643 xenografts (labadaba, p<0.0001), in kasta oo koritaanku dib u bilaabmay daawaynta ka dib.

Kaydinta

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