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Imatinib (STI571)

现货
Catalog No.
B2171
蛋白酪氨酸激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
100mg
¥ 400.00
现货

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Background

Imatinib is an inhibitor of protein-tyrosine kinase with IC50 values of 0.1, 0.1 and 0.025μM, respectively against PDGF receptor, c-Kit and Abl [1].

The type 3 group of receptor tyrosine kinases includes PDGFR, CSF-1R, Flt-3, c-Kit and so on. PDGFRs are found in normal tissues, cells as well as some tumors. It is associated with several nonmalignant proliferative diseases. In vitro assays show that Imatinib can inhibit both PDGF-AA and PDGF-BB stimulated PDGF receptor phosphorylation. Imatinib is also found to inhibit the phosphorylation of c-Kit, another kinase which mediates the growth of a number of tumors. Imatinib inhibits the phosphorylation of these kinases without effecting the expression of them. Some other kinases of the type 3 group (such as Fms and Flt-3) can’t be inhibited by Imatinib, suggesting a selectivity of Imatinib. In addition, Imatinib is shown to significantly inhibit the Bcr-Abl tyrosine kinase both in cell-based assay and in vitro kinase assay. Moreover, as a downstream pathway of PDGF-mediated signals, MAP kinase activation can also be effected in rat A10 smooth muscle cells [1].

References:
[1] Elisabeth Buchdunger, Catherine L. Cioffi, Norman Law, David Stover, Sayuri Ohno-Jones, Brian J. Druker And Nicholas B. Lydon. Abl protein-tyrosine kinase inhibitor sti571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors. The journal of pharmacology and experimental therapeutics. 2000, 295(1): 139-145.

Chemical Properties

StorageStore at -20°C
M.Wt493.6
Cas No.152459-95-5
FormulaC29H31N7O
Solubility≥24.68mg/mL in DMSO
Chemical Name4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
SDFDownload SDF
Canonical SMILESCC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

结合实验

使用Bac-to-Bac表达系统将Kdr、Flt-1、c-Met和Tek的激酶结构域在High Five细胞中表达。然后通过标准色谱技术将蛋白质纯化至接近均质。通过检测表皮生长因子受体必需的聚(Glu、Tyr)的磷酸化的降低来测量激酶的抑制作用。在优化的测定条件下(ATP浓度及Km)进行体外激酶测定。为了确定Jak-2是否被STI571抑制,将32Dp210 Bcr-Abl表达细胞血清饥饿8小时,然后用10%WEHI-3B条件培养基(IL-3来源)刺激10分钟。制备Nonidet P-40裂解物,在4°C下使用抗-Jak-2抗体(5 μl)或抗Abl抗体(20ml K12)免疫沉淀500 mg溶胞产物。免疫沉淀物与蛋白G琼脂糖结合1小时,用PBS洗涤3次,然后用激酶缓冲液洗涤3次,激酶缓冲液包含20 mM Tris、pH7.5、10 mM MgCl2、10 mM钒酸钠及1 mM二硫苏糖醇。在使用或不使用10 mM STI571条件下进行激酶测定,在10%丙烯酰胺凝胶上运行,并在磷相仪上观察。

细胞实验 [1]:

细胞系

Swiss 3T3细胞,MO7e细胞

溶解方法

该化合物在DMSO中的溶解度大于24.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

0-10 μM,90 min,37°C

应用

在Swiss 3T3细胞中,STI571预处理以剂量依赖性方式抑制PDGF-AA刺激的PDGF受体的磷酸化,IC50值约为0.1 μM。在STI571存在下,用SCF处理MO7e细胞剂量依赖性地抑制SCF刺激的酪氨酸磷酸化,IC50值约为0.1 μM。STI571抑制PDGF-BB刺激的A10细胞增殖,IC50值为0.2 μM。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1] Elisabeth Buchdunger, Catherine L. Cioffi, Norman Law, David Stover, Sayuri Ohno-Jones, Brian J. Druker And Nicholas B. Lydon. Abl protein-tyrosine kinase inhibitor sti571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors. The journal of pharmacology and experimental therapeutics. 2000, 295(1): 139-145.

生物活性

Description Imatinib (STI571)是蛋白酪氨酸激酶的选择性抑制剂,对PDGF受体、c-Kit和Abl的IC50值分别是与0.1、0.1和0.025 μM。
靶点 PDGF receptor c-Kit Abl      
IC50 0.1 μM 0.1 μM 0.025 μM      

质量控制

化学结构

Imatinib (STI571)

相关生物数据

Imatinib (STI571)

相关生物数据

Imatinib (STI571)