Poziotinib

Inoa Kimia:

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

Code 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)

Ki InChi:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Hua'ōlelo:

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

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina)

wehewehe:

ʻO Poziotinib kahi mea hoʻopaneʻe ikaika o nā kinases ʻohana EGFR me nā waiwai IC50 o 3.2, 5.3, 23.5, 4.2, a me 2.2 nM no ka wild-type EGFR, HER2, HER4, EGFRT790M, a me EGFRL858R/T790M. Loaʻa iā ia ma mua o 100- a hiki i ka 1,000-fold selectivity no EGFR kinases ma luna o 30 mau kinases i hoʻāʻo ʻia ma vitro. Hoʻopaʻa ʻo Poziotinib i ka ulu ʻana o nā ʻano ʻāhiu a me ka mutant EGFR kinase-dependent lung, ka umauma, a me nā laina cell cancer gastric (GI50s = 0.6-5.7 nM) a kāohi i ka phosphorylation EGFR a hoʻoulu i ka apoptosis in vitro. I loko o vivo, hoʻemi ka poziotinib i ka nui o ka maʻi maʻi ma ka HCC827 non-small cell lung cancer mouse xenograft model. Ke hoʻokolokolo ʻia nei nā papa hana i loaʻa ka poziotinib i nā hoʻokolohua lapaʻau no ka mālama ʻana i ka EGFR-mutant lung adenocarcinoma.

Pahuhopu: EGFR