Imatinib (STI571)
(Synonyms: 伊马替尼; STI571; CGP-57148B) 目录号 : GC10314伊马替尼 (STI571) (STI571) 是一种口服生物可利用的酪氨酸激酶抑制剂,可选择性抑制 BCR/ABL、v-Abl、PDGFR 和 c-kit 激酶活性。伊马替尼 (STI571) (STI571) 通过在 ATP 结合位点附近结合而起作用,将其锁定在封闭或自我抑制的构象中,从而半竞争性地抑制蛋白质的酶活性。伊马替尼 (STI571) 也是 SARS-CoV 和 MERS-CoV 的抑制剂。
Cas No.:152459-95-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment [1]: | |
Binding assays |
The kinase domains of Kdr, Flt-1, c-Met, and Tek were expressed in High Five cells using the Bac-to-Bac expression system. The proteins were then purified to near homogeneity by standard chromatographic techniques. Kinase inhibition was measured by detecting the decrease in phosphorylation of poly(Glu, Tyr) essential for the epidermal growth factor receptor. The in vitro kinase assays were carried out under optimized assay conditions (ATP concentration; Km). To determine whether Jak-2 was inhibited by STI571, 32Dp210 Bcr-Abl-expressing cells were serum starved for 8 h, and then stimulated for 10 min with 10% WEHI-3B-conditioned medium (IL-3 source). Nonidet P-40 lysates were prepared, and 500 mg of lysate was immunoprecipitated with either anti-Jak-2 antibodies (5 m l; Upstate Biotechnology), or anti-Abl antibodies (20 ml K12), overnight at 4°C. Immunoprecipitates were bound to protein G Sepharose for 1 h, washed three times with PBS, and then with kinase buffer (20 mM Tris, pH 7.5, 10 mM MgCl2 , 10 mM sodium vanadate, 1 mM dithiothreitol). Kinase assays were performed with or without 10 mM STI571, run on a 10% acryl-amide gel, and exposed on a phosphorimager. |
Cell experiment [1]: | |
Cell lines |
Swiss 3T3 cells, MO7e cells |
Preparation method |
The solubility of this compound in DMSO is >24.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
0-10 μM, 90 min, 37°C |
Applications |
Pretreatment of Swiss 3T3 cells with STI571 caused a dose-dependent inhibition of PDGF-AA-stimulated PDGF receptor phosphorylation with an IC50 value of ~0.1 μM. Treatment of MO7e cells with SCF in the presence of STI571 dose-dependently inhibited SCF-stimulated tyrosine phosphorylation with an IC50 value of ~0.1 μM. STI571 inhibited PDGF-BB-stimulated A10 cell proliferation with an IC50 value of 0.2 μM. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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. |
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.
Cas No. | 152459-95-5 | SDF | |
别名 | 伊马替尼; STI571; CGP-57148B | ||
化学名 | 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide | ||
Canonical SMILES | CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5 | ||
分子式 | C29H31N7O | 分子量 | 493.6 |
溶解度 | ≥ 24.68mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.0259 mL | 10.1297 mL | 20.2593 mL |
5 mM | 0.4052 mL | 2.0259 mL | 4.0519 mL |
10 mM | 0.2026 mL | 1.013 mL | 2.0259 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。