Bayani

Ribociclib (LEE01) shine takamaiman mai hana CDK4/6 tare da ƙimar IC50 na 10 nM da 39 nM, bi da bi, kuma ya wuce 1,000-ninka ƙasa da ƙarfi a kan hadaddun cyclin B/CDK1.

A cikin Vitro

Yin maganin panel na 17 neuroblastoma cell Lines tare da Ribociclib (LEE011) a cikin kewayon kashi hudu (10 zuwa 10,000 nM).Jiyya tare da Ribociclib yana hana haɓakar haɓakar haɓakar da ke da alaƙa da sarrafawa a cikin 12 na layin sel neuroblastoma 17 da aka bincika (ma'ana IC50 = 306).±68 nM, la'akari da layukan masu mahimmanci kawai, inda aka ayyana hankali azaman IC50 na ƙasa da 1μM. Ribociclib jiyya na biyu neuroblastoma cell Lines (BE2C da IMR5) tare da nuna hankali ga CDK4 / 6 hanawa sakamakon a cikin wani kashi-dogara tara kwayoyin a cikin G0 / G1 lokaci na cell sake zagayowar.Wannan kama G0/G1 ya zama mahimmanci a yawan Ribociclib na 100 nM (p=0.007) da 250 nM (p=0.01), bi da bi.

CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, m in vitro), ko EBC1 (ba a kara girma, resistant in vitro) xenografts ana bi da sau ɗaya kowace rana don kwanaki 21 tare da Ribociclib (LEE011; 200 mg / kg) ko tare da sarrafa abin hawa.An yi haƙuri da wannan dabarar dosing da kyau, saboda ba a sami asarar nauyi ko wasu alamun guba ba a cikin kowane nau'in xenograft.Ci gaban Tumor yana da jinkiri sosai a cikin kwanakin 21 na jiyya a cikin berayen da ke ɗauke da BE2C ko 1643 xenografts (duka, p<0.0001), kodayake ci gaban ya dawo bayan jiyya.

Ajiya

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