Kev piav qhia

Ribociclib (LEE01) yog ib qho tshwj xeeb CDK4/6 inhibitor nrog IC50 qhov tseem ceeb ntawm 10 nM thiab 39 nM, raws li, thiab muaj ntau dua 1,000-fold tsis muaj zog tiv thaiv cyclin B / CDK1 complex.

Hauv Vitro

Kev kho lub vaj huam sib luag ntawm 17 kab mob neuroblastoma ntawm tes nrog Ribociclib (LEE011) hla plaub-log koob ntau (10 txog 10,000 nM). Kev kho mob nrog Ribociclib ho inhibits substrate adherent kev loj hlob txheeb ze rau kev tswj nyob rau hauv 12 ntawm 17 neuroblastoma cell kab kuaj (txhais tau tias IC50 = 306±68 nM, xav txog cov kab rhiab nkaus xwb, qhov rhiab heev txhais tau tias yog IC50 tsawg dua 1μM. Ribociclib kev kho mob ntawm ob kab mob neuroblastoma ntawm tes (BE2C thiab IMR5) nrog rau kev ua kom pom tseeb ntawm CDK4/6 inhibition ua rau muaj kev cuam tshuam ntawm cov hlwb hauv G0 / G1 theem ntawm lub voj voog ntawm tes. Qhov kev ntes G0 / G1 no dhau los ua qhov tseem ceeb ntawm Ribociclib concentrations ntawm 100 nM (p = 0.007) thiab 250 nM (p = 0.01), feem.

CB17 immunodeficient nas bearing BE2C, NB-1643 (MYCN amplified, rhiab hauv vitro), lossis EBC1 (non-amplified, resistant in vitro) xenografts raug kho ib hnub ib hnub rau 21 hnub nrog Ribociclib (LEE011; 200 mg / kg) lossis nrog rau tswj tsheb. Qhov kev siv tshuaj no tau txais txiaj ntsig zoo, vim tias tsis muaj qhov hnyav lossis lwm yam cim ntawm toxicity tau pom nyob rau hauv ib qho ntawm cov qauv xenograft. Cov qog loj hlob qeeb qeeb thoob plaws hauv 21 hnub ntawm kev kho mob hauv nas harboring BE2C lossis 1643 xenografts (ob leeg, p<0.0001), txawm hais tias kev loj hlob rov qab kho tom qab kho.

Cia

Cov qauv tshuaj