Poziotinib

Lub npe tshuaj:

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

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) ib.

InChi Key:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Lo lus tseem ceeb:

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

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli)

Nqe lus piav qhia:

Poziotinib yog ib qho muaj zog inhibitor ntawm EGFR tsev neeg kinases nrog IC50 qhov tseem ceeb ntawm 3.2, 5.3, 23.5, 4.2, thiab 2.2 nM rau cov tsiaj qus EGFR, HER2, HER4, EGFRT790M, thiab EGFRL858R/T790M, hwm. Nws muaj ntau dua 100- txog 1,000-fold selectivity rau EGFR kinases tshaj 30 lwm yam kuaj kinases hauv vitro. Poziotinib inhibits kev loj hlob ntawm cov tsiaj qus thiab mutant EGFR kinase-nyob ntawm lub ntsws, lub mis, thiab kab mob qog noj ntshav hauv plab (GI50s = 0.6-5.7 nM) thiab inhibits EGFR phosphorylation thiab induces apoptosis hauv vitro. Hauv vivo, poziotinib txo cov qog loj hauv HCC827 uas tsis yog lub xov tooj ntawm tes mob ntsws cancer nas xenograft qauv. Cov qauv uas muaj poziotinib tab tom tshawb nrhiav hauv kev sim tshuaj kho mob EGFR-mutant ntsws adenocarcinoma.

Hom phiaj: EGFR