Poziotib

Sunan Sinadari:

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

Lambar SMILES:

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

Lambar 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)

InChi Key:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Mabuɗin kalma:

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

Solubility:Mai narkewa a cikin DMSO

Ajiya:0 - 4 ° C na gajeren lokaci (kwanaki zuwa makonni), ko -20 ° C na dogon lokaci (watanni)

Bayani:

Poziotinib shine mai hanawa mai ƙarfi na kinases na dangin EGFR tare da ƙimar IC50 na 3.2, 5.3, 23.5, 4.2, da 2.2 nM don nau'in EGFR, HER2, HER4, EGFRT790M, da EGFRL858R/T790M. Yana da zaɓi fiye da 100- zuwa 1,000-ninka don EGFR kinases sama da 30 sauran gwajin kinases a cikin vitro. Poziotinib yana hana ci gaban nau'in daji da mutant EGFR kinase-dogara huhu, nono, da layin kwayar cutar daji na ciki (GI50s = 0.6-5.7 nM) kuma yana hana EGFR phosphorylation kuma yana haifar da apoptosis a cikin vitro. A cikin vivo, poziotinib yana rage girman ƙwayar cuta a cikin samfurin HCC827 mara ƙaramin ƙwayar cutar kansar huhu na xenograft. Ana gudanar da gwaje-gwajen da ke ɗauke da poziotinib a cikin gwaji na asibiti don maganin EGFR-mutant huhu adenocarcinoma.

Saukewa: EGFR