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Literature DB >> 21306821

Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer.

Hyun-Jin Nam¹, Hwang-Phill Kim, Young-Kwang Yoon, Hyung-Seok Hur, Sang-Hyun Song, Maeng-Sup Kim, Gwan-Sun Lee, Sae-Won Han, Seock-Ah Im, Tae-You Kim, Do-Youn Oh, Yung-Jue Bang.

Abstract

Trastuzumab, a HER2 directed treatment has shown clinical benefit in HER2 amplified gastric cancer. This study demonstrated the potent antitumor activity of HM781-36B, a quinazoline-based irreversible pan-HER inhibitor, in HER2 amplified gastric cancer cells (SNU216 and N87) in vitro and in vivo. HM781-36B inhibited phosphorylation of HER family and downstream signaling molecules, and induced apoptosis and G1 arrest. Furthermore, HM781-36B exerted synergistic effects with chemotherapeutic agents in both HER2 amplified and HER2 non-amplified gastric cancer cells. Therefore, HM781-36B may be useful for the treatment of HER2 amplified gastric cancer alone or in combination with chemotherapeutic agents.

Entities: Chemical Disease Gene

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Year: 2011 PMID： 21306821 DOI： 10.1016/j.canlet.2011.01.010

Source DB: PubMed Journal: Cancer Lett ISSN： 0304-3835 Impact factor: 8.679

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Cited

14 in total

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