Imatinib Mesylate (STI571)
(Synonyms: 甲磺酸伊马替尼; STI571 Mesylate; CGP-57148B Mesylate) 目录号 : GC11759
An inhibitor of c-Abl, Bcr-Abl, PDGFR, and c-Kit
Cas No.:220127-57-1
Sample solution is provided at 25 µL, 10mM.
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Imatinib mesylate is a tyrosine kinase inhibitor IC50 value of 100 nM, 100 nM, 600 nM for v-Abl, c-kit, PDGFR, respectively [1].
Tyrosine kinase is an enzyme which is a subclass of protein kinase and plays an important role in transferring a phosphate group from ATP to a protein in cells. It is shown that tyrosine kinase plays a pivotal role in the management of disorders in which activation of c-Abl, PDGFR, or c-Kit signaling. Recently, the role of tyrosine kinases in the modulation of growth factor signaling are received more and more attention and gradually become an especial important target [2].
Imatinib Mesylate is a specific tyrosine kinase (abl, c-kit, and PDGFR) inhibitor and is reported to sensitize cells to radio- or chemo-therapy. When tested with Y-79 and WERI-RB-1 Rb cell lines, imatinib mesylate treatment decreased the cell proliferation and invasion with the concentration of 10 μM [3]. In osteoblast cells, administration of imatinib mesylate decreased osteoclast development via stimulating differentiation, inhibiting proliferation and survival [4].
In dog model with mast cell tumor, administration of imatinib mesylate at a dose of 10 mg/kg daily for 1-9 weeks reduced tumor growth via inhibiting tyrosine kinase [5].
References:
[1].Buchdunger, E., et al., Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class. Proc Natl Acad Sci U S A, 1995. 92(7): p. 2558-62.
[2].Zhou, Y., et al., The multi-targeted tyrosine kinase inhibitor vandetanib plays a bifunctional role in non-small cell lung cancer cells. Sci Rep, 2015. 5: p. 8629.
[3].de Moura, L.R., et al., The effect of imatinib mesylate on the proliferation, invasive ability, and radiosensitivity of retinoblastoma cell lines. Eye (Lond), 2013. 27(1): p. 92-9.
[4].O'Sullivan, S., et al., Imatinib mesylate does not increase bone volume in vivo. Calcif Tissue Int, 2011. 88(1): p. 16-22.
[5].Isotani, M., et al., Effect of tyrosine kinase inhibition by imatinib mesylate on mast cell tumors in dogs. J Vet Intern Med, 2008. 22(4): p. 985-8.
| Cell experiment: [1] | |
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Cell lines |
T cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
IC50: 3.9 μM for inhibiting DCs-stimulated T-cell proliferation 2.9 μM for inhibiting PHA-stimulated T-cell proliferation 4 days |
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Applications |
Cells were stimulated with allogeneic mature DCs or PHA in the presence of imatinib mesylate. The drug inhibited T-cell proliferation as a function of concentration. The effects were significant at 0.5 μM imatinib mesylate for the cells stimulated by DCs and at 1.0 μM imatinib mesylate for the cells stimulated with PHA. The IC50 values for imatinib mesylate–inhibited T-cell proliferation stimulated by DCs and PHA were 3.9 μM and 2.9 μM, respectively. |
| Animal experiment: [2] | |
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Animal models |
Female C57BL/6 mice |
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Dosage form |
Intraperitoneal injection, 25 or 50mg/kg/day |
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Applications |
Administration of imatinib alone did not generate any changes in lung morphology. However, when imatinib was administered in bleomycin-treated mice, a reduction of fibrotic lesions in the subpleural areas of lung was observed at doses of 25 and 50 mg/kg/day. The quantitative histologic analysis demonstrated that the fibrotic score in mice treated with bleomycin and 50 mg/kg/day of imatinib was significantly lower than that treated with bleomycin alone. The collagen content of the lung was also significantly lower in mice treated with bleomycin and imatinib (50 mg/kg/day) as compared with those treated with bleomycin alone. |
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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. |
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References: [1] Dietz A B, Souan L, Knutson G J, et al. Imatinib mesylate inhibits T-cell proliferation in vitro and delayed-type hypersensitivity in vivo. Blood, 2004, 104(4): 1094-1099. [2] Aono Y, Nishioka Y, Inayama M, et al. Imatinib as a novel antifibrotic agent in bleomycin-induced pulmonary fibrosis in mice. American journal of respiratory and critical care medicine, 2005, 171(11): 1279-1285. | |
| Cas No. | 220127-57-1 | SDF | |
| 别名 | 甲磺酸伊马替尼; STI571 Mesylate; CGP-57148B Mesylate | ||
| 化学名 | methanesulfonic acid;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.CS(=O)(=O)O | ||
| 分子式 | C29H31N7O.CH4SO3 | 分子量 | 589.71 |
| 溶解度 | ≥ 29.5mg/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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6957 mL | 8.4787 mL | 16.9575 mL |
| 5 mM | 0.3391 mL | 1.6957 mL | 3.3915 mL |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6957 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet