Title of article :
Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer
Author/Authors :
Nam، نويسنده , , Hyun-Jin and Kim، نويسنده , , Hwang-Phill and Yoon، نويسنده , , Young-Kwang and Hur، نويسنده , , Hyung-Seok and Song، نويسنده , , Sang-Hyun and Kim، نويسنده , , Maeng-Sup and Lee، نويسنده , , Gwan-Sun and Han، نويسنده , , Sae-Won and Im، نويسنده , , Seock-Ah and Kim، نويسنده , , Tae-You and Oh، نويسنده , , Do-Youn and Bang، نويسنده , , Yung-Jue and Kim، نويسنده ,
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.
Keywords :
HM781-36B , Pan-HER inhibitor , Antitumor activity , Chemotherapeutic agents , Gastric cancer
