Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Imatinib Mesylate (STI571 Mesylate) 是一种多靶点受体酪氨酸激酶抑制剂,可选择性抑制 BCR/ABL、v-Abl、PDGFR、c-kit 等激酶活性,具有口服活性。Imatinib Mesylate 具有抗肿瘤活性,可用于治疗慢性粒细胞白血病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
100 mg | ¥ 298 | 现货 | ||
200 mg | ¥ 417 | 现货 | ||
500 mg | ¥ 756 | 现货 | ||
5 g | ¥ 3,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 387 | 现货 |
产品描述 | 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. |
靶点活性 | PDGFR:0.3 μM, c-Kit:0.1 μM |
体外活性 |
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] |
体内活性 |
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] |
细胞实验 | 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]. |
动物实验 | 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]. |
别名 | 甲磺酸伊马替尼, ST-1571 Mesylate, STI-571, CGP-57148B |
分子量 | 589.71 |
分子式 | C29H31N7O·CH4SO3 |
CAS No. | 220127-57-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 59 mg/mL (100 mM)
DMSO: 50 mg/mL (84.79 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 1.6957 mL | 8.4787 mL | 16.9575 mL | 42.3937 mL |
5 mM | 0.3391 mL | 1.6957 mL | 3.3915 mL | 8.4787 mL | |
10 mM | 0.1696 mL | 0.8479 mL | 1.6957 mL | 4.2394 mL | |
20 mM | 0.0848 mL | 0.4239 mL | 0.8479 mL | 2.1197 mL | |
50 mM | 0.0339 mL | 0.1696 mL | 0.3391 mL | 0.8479 mL | |
H2O | 100 mM | 0.017 mL | 0.0848 mL | 0.1696 mL | 0.4239 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Imatinib Mesylate 220127-57-1 Angiogenesis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl PDGFR c-Kit 甲磺酸伊马替尼 inhibit ST-1571 Mesylate STI 571 STI571 CD117 Platelet-derived growth factor receptor Inhibitor STI-571 ST1571 Mesylate SCFR ST 1571 Mesylate Imatinib CGP-57148B inhibitor