Imatinib

• 产品编号：CST-9084S      品牌：CST       原厂货号：9084S
• 产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
• 应用分类：

描述：

提供的伊马替尼为冻干粉。对于10mM浓度贮存液，在5mg冻干粉中加入847.9 μl DMSO。工作浓度和处理时间根据所需的预期效果来确定，一般是1-10 μM，处理1-2小时。能溶于DMSO（100 mg/ml）和水（200 mg/ml），难溶于乙醇。伊马替尼是一种酪氨酸激酶（TK）抑制剂，是Bcr-Abl，PDGF受体和c-Kit TKs的特异性ATP结合位点拮抗物（1-3）。伊马替尼在慢性髓细胞样白血病（CML）的临床试验中结果很不错，已经成为有针对性的癌症治疗的范例（4-6）。利用磷酸化酪氨酸通路的信号传导已经被广泛研究，酪氨酸磷酸化与许多细胞生长和分化途径有关（7-9）。因为观察到的CML的状态依赖于完整的Bcr-Abl酪氨酸激酶活性，我们做了多方面的工作来确认Bcr-Abl的底物和引起髓系分化的可能机制。许多研究小组已经发现了CML胚细胞和Bcr-Abl表达细胞系（包括SHIP， c-Cbl，Dok，Shc和CrkL）中具有特征性的酪氨酸磷酸化蛋白质底物（10-15）。另外，主要的信号传导通路（包括P13激酶，Ras，Myc和Stat5）也是以Bcr-Abl激酶依赖的方式活化的（16）。

原厂资料：

Applications Key:

Molecular Characterization

C29H31N7O + CH4SO3

Purity

>99%

Directions for Use

Imatinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 847.9 μl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 1-10 μM for 1-2 hours. Soluble in DMSO at 100 mg/ml; poorly soluble in ethanol. Soluble in water at 200 mg/ml.

Background

Imatinib is a tyrosine kinase (TK) inhibitor that is a relatively specific ATP-binding site antagonist of Bcr-Abl, PDGF receptor, and c-Kit TKs (1-3). Results are encouraging in chronic myeloid leukemia (CML) clinical trials and imatinib has become a paradigm for targeted cancer therapeutics (4-6). Signal transduction through phospho-tyrosine pathways has been studied extensively, and tyrosine phosphorylation has been linked to multiple cell growth and differentiation pathways (7-9). Because the observed leukemic state of CML is dependent on the intact Bcr-Abl tyrosine kinase activity, extensive work has been done to identify substrates of Bcr-Abl and thus possible mechanisms leading to a myeloid expansion. Many groups have characterized prominent tyrosine-phosphorylated protein substrates in both CML blasts and Bcr-Abl-expressing cell lines, including SHIP, c-Cbl, Dok, Shc, and CrkL (10-15). In addition, key signal transduction pathways involving PI3 kinase, Ras, Myc, and Stat5 are also activated in a Bcr-Abl kinase-dependent manner (16).

注意事项：

Storage: Store lyophilized or in solution at -20°C, desiccated.
Protect from light. In lyophilized form, the chemical is stable for
24 months. Once in solution, use within 3 months to prevent loss
of potency. Aliquot to avoid multiple freeze/thaw cycles.