Imatinib Mesylate (STI571 Mesylate) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib Mesylate has antitumor activity for the treatment of chronic granulocytic leukemia.

c-Kit:0.1 μM, PDGFR:0.3 μM

方法：人、小鼠和大鼠的骨肉瘤细胞用 Imatinib Mesylate (1-40 µM) 处理 72 h，使用 XTT assay 检测细胞活力。
结果：Imatinib 以剂量依赖性方式降低了活骨肉瘤细胞的数量，72 h 的 IC50 为：20 µM (MG-63)、11 µM (HOS)、23 µM (MOS-J)、15 µM (POS-1)、9 μM (OSRGA）。[1]
方法：人胃癌细胞 AGS、MKN45 和 SNU638 用 Imatinib Mesylate (30-100 µM) 处理 48 h，使用 Flow Cytometry 检测细胞凋亡情况。
结果：Annexin V/PI-positive 细胞的百分比显著增加，表明 Imatinib 治疗增加了肿瘤细胞的早期凋亡。[2]

方法：为研究抗肿瘤活性，将 Imatinib Mesylate (25-100 mg/kg) 口服给药给携带未分化 POS-1 或混合成骨细胞/溶骨 MOS-J 骨肉瘤肿瘤的小鼠，每天一次，持续 21 或 43 天。
结果：Imatinib 在体内抑制骨肉瘤的进展。[1]
方法：为研究对多发性硬化症 (MS) 的作用，将 Imatinib Mesylate (60 mg/kg) 口服给药给 EAE C57BL/6 小鼠模型，每周六次，持续两周。
结果：Imatinib 通过减轻疾病的严重程度和延迟发病，对 EAE 有有益的影响。Imatinib 及其潜在的治疗作用和免疫调节特性可被考虑用于治疗多发性硬化症。[3]

Cells were added to 96-well plates at a density of 20?000 cells/well for HMC-1 and 50?000 cells/well for M-07e. Experiments with M-07e were performed with the use of GM-CSF or SLF as a growth factor supplement. Experiments using HMC-1 were performed without growth factor supplementation. Proliferation at 48 hours was measured with an XTT-based assay [1].

Heterozygous experimental TRAMP mice were obtained by breeding wild-type C57BL/6 male mice and heterozygous female TRAMP mice. MC-deficient C57BL/6-KitW-sh/W-sh mice were intercrossed over 12 generations with TRAMP mice to obtain MC-deficient KitWsh-TRAMP mice. Cromolyn (10 mg/kg dissolved in saline; Sigma Aldrich) or imatinib (50 mg/kg dissolved in saline) were administered intraperitoneally in TRAMP mice for 5 days/week. Treatments started at 8 or 16 weeks, as indicated in text and figures, and continued for the duration of the experiment. Mice were sacrificed at 25 weeks and their urogenital apparatus collected for IHC [4].