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IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities.

Abstract：

:Accumulating evidence suggested that the irreversible tyrosine kinase inhibitors (TKIs) have potential to override the acquired resistance to target-based therapies. Herein, we reported IC-4 as a novel irreversible TKI for epidermal growth factor receptor (EGFR). IC-4 potentially suppressed proliferation, induced apoptosis and a G2/M cell cycle arrest in breast cancer cells, correlating with inhibition of EGF-induced EGFR activation, but independent of DNA damage. In addition, IC-4 exhibited anti-angiogenetic activities both in vitro and in vivo. It suppressed cell viability and proliferation induced by various growth factors in human umbilical vein endothelial cells (HUVECs). IC-4 also inhibited HUVECs migration and tube formation. In transgenic zebrafish embryo model, IC-4 was shown to suppress formation of intersegmental vessel and development of subintestinal vessels. Taken together, these results demonstrated that IC-4 is a new irreversible EGFR-TKI, exhibiting potent anti-breast cancer and anti-angiogenetic effects.

journal_name

Cancer Lett

journal_title

Cancer letters

authors

Li YB,Wang ZQ,Yan X,Chen MW,Bao JL,Wu GS,Ge ZM,Zhou DM,Wang YT,Li RT

doi

10.1016/j.canlet.2013.07.005

subject

Has Abstract

pub_date

2013-10-28 00:00:00

pages

88-96

issue

1

eissn

0304-3835

issn

1872-7980

pii

S0304-3835(13)00510-7

journal_volume

340

pub_type

杂志文章

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