Poziotinib

Igoa vaila'au:

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

SMILES Code:

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

InChi Code:

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

upu autu:

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

Solubility:Solu i le DMSO

Teuina:0 - 4°C mo taimi pupuu (aso i vaiaso), po'o le -20°C mo taimi uumi (masina)

Fa'amatalaga:

Poziotinib o se inhibitor malosi o EGFR aiga kinases ma IC50 tau o 3.2, 5.3, 23.5, 4.2, ma 2.2 nM mo vao-ituaiga EGFR, HER2, HER4, EGFRT790M, ma EGFRL858R / T790M, faasologa. E sili atu nai lo le 100- i le 1,000-filifili filifili mo EGFR kinases i luga ole 30 isi kinases suʻeina in vitro. Poziotinib taofia le tuputupu aʻe o le vao-ituaiga ma mutant EGFR kinase-faalagolago mama, susu, ma gastric sela sela sela (GI50s = 0.6-5.7 nM) ma taofia EGFR phosphorylation ma faaosofia apoptosis in vitro. I vivo, poziotinib fa'aitiitia le lapopo'a o le tuma i le HCC827 e le o se tama'i sela o le kanesa mama o le mama xenograft fa'ata'ita'iga. O faʻasologa o loʻo iai le poziotinib o loʻo suʻesuʻeina i suʻesuʻega faʻapitoa mo togafitiga o le EGFR-mutant lung adenocarcinoma.

Sini: EGFR