Bayani

Niraparib (MK-4827) mai ƙarfi ne mai ƙarfi kuma mai hanawa ta baki PARP1 da mai hanawa PARP2 tare da IC50s na 3.8 da 2.1 nM, bi da bi.Niraparib yana haifar da hana gyare-gyaren lalacewar DNA, yana kunna apoptosis kuma yana nuna ayyukan anti-tumor.

A cikin Vitro

Niraparib (MK-4827) yana hana ayyukan PARP tare da EC50 = 4 nM da EC90 = 45 nM a cikin dukkanin kwayoyin halitta.MK-4827 yana hana yaduwar kwayoyin cutar kansa tare da mutant BRCA-1 da BRCA-2 tare da CC50 a cikin kewayon 10-100 nM.MK-4827 yana nuna ingantacciyar PARP 1 da 2 hanawa tare da IC50 = 3.8 da 2.1 nM, bi da bi, kuma a cikin cikakken gwajin kwayar halitta[1].Don tabbatar da cewa Niraparib (MK-4827) yana hana PARP a cikin waɗannan layin tantanin halitta, ana kula da ƙwayoyin A549 da H1299 tare da 1.μM MK-4827 na lokuta daban-daban da kuma auna ayyukan PARP enzymatic ta amfani da gwajin chemiluminescent.Sakamakon ya nuna cewa Niraparib (MK-4827) ya hana PARP a cikin minti na 15 na jiyya ya kai kusan 85% hanawa a cikin sel A549 a 1 h da kusan 55% hanawa a 1 h don ƙwayoyin H1299.

Niraparib (MK-4827) an jure shi sosai kuma yana nuna inganci azaman wakili ɗaya a cikin ƙirar xenograft na ƙarancin ciwon daji na BRCA-1.Niraparib (MK-4827) an jure shi sosai a cikin vivo kuma yana nuna inganci azaman wakili ɗaya a cikin ƙirar xenograft na ƙarancin ciwon daji na BRCA-1.Niraparib (MK-4827) an kwatanta shi ta hanyar pharmacokinetics mai karɓa a cikin berayen tare da izinin plasma na 28 (mL / min) / kg, babban adadin rarraba (Vd)_ss= 6.9 L/kg), tsawon rabin rayuwa (t_1/2= 3.4 h), da kuma kyakkyawan bioavailability, F = 65%^[1].Niraparib (MK-4827) yana haɓaka amsawar radiation na p53 mutant Calu-6 tumor a cikin lokuta biyu, tare da kashi ɗaya na yau da kullum na 50 mg / kg yana da tasiri fiye da 25 mg / kg da aka ba sau biyu kowace rana.^].

Ajiya

Tsarin sinadaran