Receptor tyrosine kinase inhibitors (RTKIs) has been found to be a potential candidate for the treatment of hepatocellular carcinoma.We have synthesized a novel series compounds as inhibitors of tyrosine kinases serine kinases.The objective of this research is to evaluate the efficacy and safety of BZG-4000. In vitro study determined 50% inhibition concentration (IC₅₀) of nine compounds on ten human cancer cell lines using MTS assay. The cells were harvested respectively during the logarithmic growth period and counted with hemocytometer. The plate was incubated for 1-4 hours at 37 °C in a humidified, 5% CO₂ atmosphere. The absorbance at 490 nm was recorded using SpectraMAX Plus microplate spectrophotometer. BZG-4000 005 was elected for in vivo study. Huh-7 cells were injected subcutaneously into nude mice to observe in vivo tumor growth. Inhibition rate of tumor volume was calculated. The results of IC₅₀ of test articles on ten human cancer cell lines in MTS assay shown BZG-4000 005 inhibited the growth of three cell lines of liver cancer with doses from 0.01 µM up to 28.25µM. In addition, compared with the positive control drug, BZG-4000 005 significantly inhibited Huh-7 cell-derived tumor xenografts in Balb/c nude mice. In conclusion, BZG-4000 may be a potential and promising agent to treat liver cancer.