Tsanangudzo

Niraparib (MK-4827) ine simba zvakanyanya uye nemuromo bioavailable PARP1 uye PARP2 inhibitor ine IC50s ye3.8 uye 2.1 nM, zvichiteerana. Niraparib inotungamira mukudzivirirwa kwekugadzirisa kwekukuvara kweDNA, inomutsa apoptosis uye inoratidza anti-bundu chiitiko.

In Vitro

Niraparib (MK-4827) inhibisa PARP chiitiko neEC50=4 nM uye EC90=45 nM mune yesero yesero assay. MK-4827 inhibisa kuwanda kwekenza maseru ane mutant BRCA-1 uye BRCA-2 ine CC50 mune 10-100 nM renji. MK-4827 inoratidza yakanakisa PARP 1 uye 2 inhibition ine IC50=3.8 uye 2.1 nM, zvichiteerana, uye mune yesero yesero assay[1]. Kusimbisa kuti Niraparib (MK-4827) inhibits PARP mumasero aya, A549 uye H1299 masero anobatwa ne1.μM MK-4827 kwenguva dzakasiyana uye yakayera PARP enzymatic chiitiko uchishandisa chemiluminescent assay. Zvigumisiro zvinoratidza kuti Niraparib (MK-4827) inodzivisa PARP mukati memaminitsi e15 ekurapa anosvika anenge 85% inhibition mumasero eA549 pa1 h uye inenge 55% inhibition pa 1 h yeH1299 masero.

Niraparib (MK-4827) inoshivirirwa zvakanaka uye inoratidza kushanda senge mumiriri mumwechete mune xenograft modhi yeBRCA-1 isina kukwana cancer. Niraparib (MK-4827) inoshivirirwa zvakanaka mu vivo uye inoratidza kushanda semumiriri mumwechete mune xenograft modhi yeBRCA-1 isina kukwana cancer. Niraparib (MK-4827) inoratidzirwa ne pharmacokinetics inogamuchirwa mumakonzo ane plasma clearance ye 28 (mL/min)/kg, yakakwira kwazvo kugovera (Vd)._ss= 6.9 L/kg), refu terminal hafu yeupenyu (t_1/2=3.4 h), uye yakanakisa bioavailability, F=65%^[1]. Niraparib (MK-4827) inosimudzira mhinduro yemwaranzi yep53 mutant Calu-6 tumor muzviitiko zvese izvi, ine imwechete yezuva nezuva ye50 mg/kg ichinyanya kushanda kupfuura 25 mg/kg inopiwa kaviri zuva nezuva.^].

Storage

Chimiro chemakemikari