Poziotib

Orukọ Kemikali:

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

KỌỌDỌ SMILES:

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

Koodu 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)

Bọtini InChi:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu)

Apejuwe:

Poziotinib jẹ oludena ti o lagbara ti awọn kinases idile EGFR pẹlu awọn iye IC50 ti 3.2, 5.3, 23.5, 4.2, ati 2.2 nM fun EGFR-iru-ẹgan, HER2, HER4, EGFRT790M, ati EGFRL858R/T790M. O ni o tobi ju 100- si 1,000-agbo selectivity fun EGFR kinases lori 30 miiran idanwo kinases ni fitiro. Poziotinib ṣe idiwọ idagbasoke ti iru-igi ati mutant EGFR kinase-ti o gbẹkẹle ẹdọfóró, igbaya, ati awọn laini sẹẹli alakan inu (GI50s = 0.6-5.7 nM) ati ṣe idiwọ EGFR phosphorylation ati fa apoptosis in vitro. Ni vivo, poziotinib dinku iwọn tumo ninu awoṣe HCC827 ti kii-kekere sẹẹli akàn ẹdọfóró asin xenograft. Awọn agbekalẹ ti o ni poziotinib wa labẹ iwadii ni awọn idanwo ile-iwosan fun itọju adenocarcinoma ẹdọfóró EGFR-mutant.

afojusun: EGFR