It is generally accepted that the occurrence and development of cancer are closely related to tumor angiogenesis. Vascular endothelial growth factor and its receptor(VEGF/VEGFR)signal pathway plays an important role in regulating and controlling angiogenesis,and is also the key target of many kinds of anti-angiogenesis drugs. Mesylate apatinib is a new and small molecular anti-angiogenesis drug,which can strongly against tumor angiogenesis by inhibiting VEGFR-2 with highly selectivity. A series of clinical trials confirms that there were certain objective response and obvious survival benefit to advanced gastric cancer patients treated by apatinib, who failed in the standard chemotherapy,also with better safety. Currently, trials and clinical studies of apatinib alone or in combination with other drugs for lung cancer, hepatic cancer, gastric cancer, colorectal cancer and breast cancer are carried on. This article reviewed fundamental experiments and clinical trials to provide reference for further using of apatinib in clinic.