Poziotinib

Chemical Name:

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

SMILES Kodhi:

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)

InChi Key:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Keyword:

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

Solubility:Soluble muDMSO

Kuchengeta:0 - 4 ° C kwenguva pfupi (mazuva kusvika mavhiki), kana -20 ° C kwenguva refu (mwedzi)

Tsanangudzo:

Poziotinib inhibitor yakasimba yeEGFR family kinases ine IC50 tsika dze 3.2, 5.3, 23.5, 4.2, uye 2.2 nM yemhando yemhuka EGFR, HER2, HER4, EGFRT790M, uye EGFRL858R/T790M, maererano. Iine yakakura kudarika 100- kusvika ku1,000-fold selectivity yeEGFR kinases pamusoro pe 30 mamwe kinases akaedzwa mu vitro. Poziotinib inhibits kukura kwemusango-rudzi uye mutant EGFR kinase-inotsamira mapapu, mazamu, uye gastric cancer cell mitsara (GI50s = 0.6-5.7 nM) uye inhibits EGFR phosphorylation uye induces apoptosis in vitro. Mu vivo, poziotinib inoderedza bundu saizi muHCC827 isiri-diki yesero kenza yemapapu mbeva xenograft modhi. Magadzirirwo ane poziotinib ari pasi pekuongororwa mumakiriniki ekuedzwa kwekurapa kweEGFR-mutant lung adenocarcinoma.

Chinangwa: EGFR