TY - JOUR AU - Chen Zhuo AU - Tong Lin-jiang AU - Tang Bai-you AU - Liu Hong-yan AU - Wang Xin AU - Zhang Tao AU - Cao Xian-wen AU - Chen Yi AU - Li Hong-lin AU - Qian Xu-hong AU - Xu Yu-fang AU - Xie Hua AU - Ding Jian PY - 2019 TI - C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis JF - Acta Pharmacologica Sinica; Vol 40, No 6 (June 2019): Acta Pharmacologica Sinica Y2 - 2019 KW - N2 - The fibroblast growth factor receptors (FGFRs) are increasingly considered attractive targets for therapeutic cancer intervention due to their roles in tumor metastasis and angiogenesis. Here, we identified a new selective FGFR inhibitor, C11, and assessed its antitumor activities. C11 was a selective FGFR1 inhibitor with an IC 50 of 19 nM among a panel of 20 tyrosine kinases. C11 inhibited cell proliferation in various tumors, particularly bladder cancer and breast cancer. C11 also inhibited breast cancer MDA-MB-231 cell migration and invasion via suppression of FGFR1 phosphorylation and its downstream signaling pathway. Suppression of matrix metalloproteinases 2/9 (MMP2/9) was associated with the anti-motility activity of C11. Furthermore, the anti-angiogenesis activity of C11 was verified in endothelial cells and chicken chorioallantoic membranes (CAMs). C11 inhibited the migration and tube formation of HMEC-1 endothelial cells and inhibited angiogenesis in a CAM assay. In sum, C11 is a novel selective FGFR1 inhibitor that exhibits potent activity against breast cancer metastasis and angiogenesis. UR - http://www.chinaphar.com/article/view/9983