| 名称 | Imatinib |
| 描述 | Imatinib (STI571) 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 has antitumor activity for the treatment of chronic granulocytic leukemia. |
| 细胞实验 | M-07e cells were grown in serum-free RPMI 1640 at 37°C for approximately 18 hours before they were incubated for 90 minutes in the presence of various concentrations of STI 571. The cells were then pelleted and resuspended in 1 mL RPMI 1640. STI 571 was added to each tube to achieve the same concentration used during the 90 minutes of preincubation. The cells were then incubated with inhibitor and growth factor (SLF or GM-CSF) for 15 minutes at 37°C. Subsequently, the cell pellets were lysed with 100 to 250 μL of protein lysis buffer (50 mmol/L Tris, 150 mmol/L sodium chloride, 1% NP-40, and 0.25% deoxycholate, with addition of the inhibitors aprotinin, leupeptin, pepstatin, phenylmethyl sulfonyl fluoride, and sodium orthovanadate). Western immunoblot analysis was performed as previously described.41Experiments with HMC-1 cells were performed in the same way except that neither SLF nor GM-CSF was added [1]. |
| 动物实验 | Swiss mice (nu/nu, female), weighing 30 g, 6 – 8 weeks old, were bred in the animal facilities, maintained under specific pathogen-free conditions with artificial lighting (12 hr light/12 hr dark cycle) and fed a regular diet and water ad libitum. For therapeutic trials, the tumor-bearing mice were randomly divided into equivalent groups of 5 to 12 animals and mice were treated as soon as the xenografted tumors reached a diameter of 5 mm (or a tumor volume of approximately 60 mm^3). Four different human tumors were used: the SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers. STI571 was administered at a total dosage of 70 or 100 mg/kg per day in 1 or 2 intraperitoneal injections, with or without etoposide plus ifosfamide or topotecan. STI571 was diluted in 150 l of H2O and administered on different days, as indicated. Etoposide and ifosfamide were diluted in 200 l of 0.9% sodium chloride, and topotecan was diluted in 150 l of 0.9% sodium chloride. The control group received injections according to the same schedule as experimentally treated mice. All mice were weighed once weekly. Tumor growth was monitored by measuring 2 perpendicular diameters with calipers. Tumor volume (V) and the relative tumor volume (RTV) were calculated as:. V = a^2 × b/2,. where a is the width (large diameter) and b the length (small. diameter) of the tumor in millimeters, and. RTV = Vx/Vi,. where Vx is the mean tumor volume in cubic millimeters at any given time and Vi is the mean initial tumor volume in cubic millimeters at the start of treatment. Mice were ethically sacrificed when the tumor volume reached 2,500 mm^3 [5]. |
| 体外活性 | 方法：人、小鼠和大鼠的骨肉瘤细胞用 Imatinib (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 (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] |
| 体内活性 | 方法：为研究抗肿瘤活性，将 Imatinib (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 (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] |
| 存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.5 mg/mL (5.06 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 25 mg/mL (50.65 mM)
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| 关键字 | Autophagy | CGP-57148B | Platelet-derived growth factor receptor | SCFR | c-Kit | Inhibitor | ST 1571 | SARS coronavirus | STI 571 | inhibit | CD117 | PDGFR | ST1571 | STI-571 | SARS-CoV | Bcr-Abl | Imatinib |
| 相关产品 | Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Hydroxychloroquine | Curcumin | Stavudine | Salicylic acid | Paeonol | Sodium 4-phenylbutyrate |
| 相关库 | 抑制剂库 | 抗癌上市药物库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 抗病毒库 | FDA 上市药物库 | 药物功能重定位化合物库 | FDA 上市激酶抑制剂库 | 抗癌药物库 |