SIM-010603 (Tafetinib) is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM-010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM-010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis. SIM-010603 inhibited tumor growth in these xenograft tumor growth models. SIM010603 reduced tumor MVD in T241-VEGF-A tumor xenograft models and decreased positive signals of CD31, NG2 in MDA-MB-435, and LLC-SW-44 xenograft tumor models. SIM-010603 was in development by Simcere Pharmaceutical Group for the cancer treatment. It was in phase I clinical trials by Simcere, Jilin Boda Pharma and Nanjing Yoko Biological Pharma for the treatment of solid tumours, but this research was discontinued.