Abstract: Objectives ： To investigate receptor tyrosine kinase STI571, its regulation of tumor bio-functions on human glioblastoma cells. Methods ： The expression of PDGF and receptors were detected by immunocytochemistry; MTT assays /Soft agar colony formation assays were performed to determine the tumor cell growth/colony formation inhibition under STI571, Temozolomide (TMZ), alone and incombination; Synergy was evaluated by Chou-Talalay method; Flow cytometric assays were carried out to discover the tumor cell death induced by STI571. Immuno -blot based kinase screening was performed on some cells. Results ： 10 (M or above STI571 can completely or partial inhibit glioma cell growth and colony formation, respectively. STI571 and T MZ are synergic on inhibiting T98G growth, not the others; Higher concentration STI571 induced mixed apoptosis or necrosis; In addition, protein kinase screen indicated STI571 resistant T98G more active of cell cycle progression. Conclusion : STI571 shows considerable activity against malignant glioma cells and may act synergistically with chemotherapy drugs.