Poziotinib

Nomen chemicum:

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

SMILES Code:

C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C)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

Keyword:

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

Solubilitas:Solutum in DMSO

Repono:0 - 4° C pro brevi termino (dies ad hebdomades), vel -20° C ad terminum longum (menses)

Descriptio:

Poziotinib potens est inhibitor familiae EGFR cognationum cum valoribus IC50 3.2, 5.3, 23.5, 4.2, et 2.2 nm pro generis silvestribus EGFR, HER2, HER4, EGFRT790M, et EGFRL858R/T790M, respective. Habet maiorem quam 100- ad 1,000 duplicem selectivam pro EGFR kinases supra 30 alias probatas in vitro. Poziotinib incrementum generis silvestrium inhibet et mutant EGFR kinasum dependens pulmonem, pectus, et cancer cellae gastricae (GI50s = 0.6-5.7 nM) et phosphorylationem EGFR vetat et apoptosin in vitro inducit. In vivo, poziotinib magnitudinem tumoris minuit in exemplari HCC827 non-parvus pulmonis cellae cancri mus xenografi exemplar. Formulae poziotinib continentur quaesitae in iudiciis clinicis ad tractationem pulmonis adenocarcinoma EGFR-mutantis.

Target: EGFR