Poziotinib

Ingoa matū:

1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one

Waehere SMILES:

C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O

Waehere InChi:

InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27- 12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27 ,28,29)

Kī InChi:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Kupumatua:

Poziotinib, HM-781-36, HM-781-36B, NOV-1201, NOV-120101, 1092364-38-9

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama)

Whakaahuatanga:

Ko te Poziotinib he aukati kaha o nga kinases whanau EGFR me nga uara IC50 o 3.2, 5.3, 23.5, 4.2, me 2.2 nM mo te momo mohoao EGFR, HER2, HER4, EGFRT790M, me EGFRL858R / T790M, ia. He nui ake i te 100- ki te 1,000-fold te whiriwhiringa mo te EGFR kinases neke atu i te 30 atu kinases i whakamatauria in vitro. Ko te Poziotinib te aukati i te tipu o te momo mohoao me te mutant EGFR kinase-whakawhirinaki i te huhu, te uma, me nga raina pūtau mate pukupuku pekitīlia (GI50s = 0.6-5.7 nM) me te aukati i te phosphorylation EGFR me te whakaoho i te apoptosis in vitro. I roto i te vivo, ka whakaitihia e te poziotinib te rahi o te puku i roto i te tauira xenograft kiore o te kiore HCC827 kore-iti. Ko nga hanganga kei roto poziotinib kei te tirotirohia i roto i nga whakamatautau haumanu mo te maimoatanga o te EGFR-mutant lung adenocarcinoma.

Whāinga: EGFR