I-Poziotinib

Igama Lekhemikhali:

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

Ikhodi ye-SMILES:

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

Ikhodi ye-InChi:

I-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)

I-InChi Key:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga)

Incazelo:

I-Poziotinib iyi-inhibitor enamandla ye-EGFR family kinases enamanani e-IC50 we-3.2, 5.3, 23.5, 4.2, kanye ne-2.2 nM yohlobo lwasendle i-EGFR, HER2, HER4, EGFRT790M, kanye ne-EGFRL858R/T790M ngokulandelanayo. Inokukhetha okuphindwe ka-100 kuya kwezingu-1,000 kwe-EGFR kinases ngaphezu kwamanye ama-kinases ahloliwe angama-30 ku-vitro. I-Poziotinib ivimbela ukukhula kohlobo lwasendle kanye ne-mutant EGFR kinase-dependent lung, ibele, nemigqa yeseli yomdlavuza wesisu (GI50s = 0.6-5.7 nM) futhi ivimbela i-EGFR phosphorylation futhi ibangele i-apoptosis in vitro. Ku-vivo, i-poziotinib yehlisa usayizi wesimila kumodeli ye-xenograft yegundane yegundane ye-HCC827 engeyona encane yeseli elincane. Amafomula aqukethe i-poziotinib angaphansi kophenyo ezivivinyweni zokwelashwa zokwelashwa kwe-EGFR-mutant lung adenocarcinoma.

Ithagethi: EGFR