Home CONTACT Neoplasma 2014 Neoplasma Vol.61, No.5, p.514-522, 2014

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Founded: 1954
ISSN 0028-2685
ISSN 1338-4317 (online)

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Neoplasma Vol.61, No.5, p.514-522, 2014

Title: SKLB-287, a novel oral multikinase inhibitor of EGFR and VEGFR2, exhibits potent antitumor activity in LoVo colorectal tumor model
Author: X. CHEN, Y. LIU, H.-W. YANG, S. ZHOU, C. CHENG, M.-W. ZHENG, L. ZHONG, X.-Y. FU, Y.-L. PAN, S. MA, Y. TANG, Y.-Z. CHEN, L.-L. LI, S.-Y. YANG

Abstract: Colorectal cancer (CRC) is the third common cancer and most of the chemotherapies of CRC currently used often suffer limited efficacy and large side effects. Targeted small-molecule by anti-tumor drugs are thought a promising strategy for improving the efficacy and reducing the side effects. In this investigation, we report a novel multikinase inhibitor, termed SKLB-287, which was discovered by us recently. SKLB-287 could efficiently inhibit the activation of endothelial growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR2). It displayed very good anti-proliferative activity against LoVo CRC cells and considerable antiangiogenic potency in transgenic zebrafish embryos. Oral administration of SKLB-287 resulted in dose-dependent suppression of tumor growth in LoVo xenograft mouse model. Immunohistochemistry was adopted to examine the in vivo anti-tumor mechanism of action of SKLB-287.

Keywords: SKLB-287, EGFR, antiangiogenesis, colorectal cancer
Published online: 16-Jul-2014
Year: 2014, Volume: 61, Issue: 5 Page From: 514, Page To: 522

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