Nkọwa

Ribociclib (LEE01) bụ onye na-egbochi CDK4/6 nke ukwuu nwere ụkpụrụ IC50 nke 10 nM na 39 nM, n'otu n'otu, ma karịa 1,000-fold obere ike megide mgbagwoju cyclin B/CDK1.

Na Vitro

Na-emeso otu panel nke ahịrị sel neuroblastoma 17 na Ribociclib (LEE011) gafere ọnụọgụ ọnụọgụ anọ (10 ruo 10,000 nM).Ọgwụgwọ na Ribociclib na-egbochi uto na-adịgide adịgide maka njikwa na 12 nke ahịrị sel neuroblastoma 17 nyochara (pụtara IC50=306).±68 nM, na-atụle naanị ahịrị nwere mmetụta, ebe akọwara uche dị ka IC50 nke na-erughị 1μM. Ribociclib ọgwụgwọ nke abụọ neuroblastoma cell ahịrị (BE2C na IMR5) na-egosipụta mmetụta uche na CDK4 / 6 mgbochi na-eme ka a dose-dabere mkpokọta nke mkpụrụ ndụ na G0 / G1 nkeji nke cell okirikiri.Njide G0/G1 a na-aghọ ihe dị ịrịba ama na nchịkọta Ribociclib nke 100 nM (p=0.007) na 250 nM (p=0.01), n'otu n'otu.

CB17 immunodeficient ụmụ oke na-ebu BE2C, NB-1643 (MYCN amplified, sensitive in vitro), ma ọ bụ EBC1 (na-abụghị amplified, eguzogide in vitro) xenografts na-emeso otu ugboro kwa ụbọchị maka ụbọchị 21 na Ribociclib (LEE011; 200 mg / kg) ma ọ bụ na a njikwa ụgbọ ala.A nabatara usoro onunu ogwu a nke ọma, n'ihi na ọ nweghị mbelata ibu ma ọ bụ ihe ịrịba ama ndị ọzọ nke nsi na-ahụ n'ụdị ọ bụla nke xenograft.Ọganihu Tumor na-egbu oge n'ime ụbọchị 21 nke ọgwụgwọ na ụmụ oke na-eburu BE2C ma ọ bụ 1643 xenografts (ha abụọ, p<0.0001), n'agbanyeghị na uto maliteghachiri ọgwụgwọ mgbe ọgwụgwọ gasịrị.

Nchekwa

Ọdịdị chemical