Descriptio

Niraparib (MK-4827) plurimum valet et oretenus bioavailable PARP1 et PARP2 inhibitor cum IC50s 3.8 et 2.1 nM, respective.Niraparib ducit ad inhibitionem damni reparationis DNA, apoptosim operatur et actionem anti-tumorem ostendit.

In vitro

Niraparib (MK-4827) actio PARP vetat cum EC50=4 nM et EC90=45 nM in cellula integra.MK-4827 vetat multiplicatio cellularum cancri cum mutant BRCA-1 et BRCA-2 cum CC50 in 10-100 nm.MK-4827 praeclara PARP 1 et 2 inhibitionis cum IC50=3.8 et 2.1 nM, respective, et in tota cellula primordium [1].Ad convalidandum Niraparib (MK-4827) in his lineis cellulis PARP vetat, A549 et H1299 cum 1 cellulis tractantur.μM MK-4827 variis temporibus activitatis enzymaticae PARP mensurata utens chemiluminescenti primordium.Eventus demonstrant Niraparib (MK-4827) PARP vetare intra 15 minuta curationis attingentia circa 85% inhibitionem in cellulis A549 ad 1 h et 55% inhibitionem circa 1 h pro cellis.

Niraparib (MK-4827) bene toleratur et efficaciam demonstrat sicut unum agens in exemplari xenografo BRCA-1 cancer deficientis.Niraparib (MK-4827) bene in vivo toleratur et efficaciam demonstrat tamquam unum agens in exemplari xenografo BRCA-1 carcinomatis deficientis.Niraparib (MK-4827) notatur acceptis pharmacokineticis in muribus plasmatis alvi 28 (mL/min)/kg, altissimum volumen distributionis (Vd._ss= 6.9 L/kg), longus terminus vita dimidia (t_1/2= 3.4 h), et praestantia bioavailability, F=65%.^[1].Niraparib (MK-4827) responsio radialem auget tumorem Calu-6 mutant p53 utrobique, cum unica dosis 50 mg/kg efficacior quam 25 mg/kg data bis in die.^].

Repono

Chemical structure