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Imatinib Mesylate

产品编号 T1621 CAS 220127-57-1

别名: 甲磺酸伊马替尼, ST-1571 Mesylate, STI-571, CGP-57148B

Imatinib Mesylate (STI-571) 是一种酪氨酸激酶受体抑制剂，具有抗肿瘤活性，对 v-Abl、c-Kit 和 PDGFR 的 IC50 分别为 0.6 μM、0.1 μM 和 0.1 μM。

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Imatinib Mesylate, CAS 220127-57-1

规格	价格/CNY	货期
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

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其他形式的 Imatinib Mesylate:

选择批次

纯度: 100%

纯度: 99.73%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).
靶点活性	c-Kit:0.1 μM, PDGFR:0.3 μM
体外活性	Inhibition of Steel factor (SLF)-induced c-kit autophosphorylation by STI 571 was dose-dependent, with complete inhibition observed at both 10 and 1.0 μmol/L. Inhibition was also apparent at a dose of 0.5 μmol/L, although limited c-kit autophosphorylation still occurred. Complete inhibition of MAP kinase activation occurred at 10- and 1.0-μmol/L concentrations of STI 571. Partial inhibition was observed at a dose of 0.1 μmol/L, and no inhibition occurred at a dose of 0.01 μmol/L. Total MAP kinase expression was not altered by treatment with STI 571 [1]. Exposure of cells to 1 μM STI571 for 24 hours before lysis resulted in a reduction of cellular tyrosine phosphorylation in general and of TEL/ARG specifically [2]. Imatinib had a more similar effect on Bcr/Abl- and c-Kit–dependent proliferation, with an IC50 of 19 nM in R10(-) cells and 82 nM in MO7e cells growing in the presence of SCF (KL, Kit ligand), respectively [3].
体内活性	The treatment of imatinib significantly reduced the incidence of adenocarcinomas (47.1% vs. 76.9% of untreated TRAMP mice) but had no effect against NE tumors, which instead significantly increased in frequency (23.5% vs. 15.4% of untreated TRAMP mice) [4]. In the imatinib group, lung function was improved with a lower W/D ratio. Perivascular edema and neutrophil infiltration were ameliorated. The imatinib group demonstrated maintained expression of VEC, inhibition of pCrkL, and a significantly higher level of interleukin (IL)-10 [5].
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 59 mg/mL (100 mM)

DMSO: 59 mg/mL (100 mM)

溶液配制表

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
	100 mM	0.017 mL	0.0848 mL	0.1696 mL	0.4239 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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参考文献

1. Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32. 2. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8 3. Wolff NC, et al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood. 2005 May 15;105(10):3995-4003. 4. Jachetti E, et al. Imatinib Spares cKit-Expressing Prostate Neuroendocrine Tumors, whereas Kills Seminal Vesicle Epithelial-Stromal Tumors by Targeting PDGFR-β. Mol Cancer Ther. 2017 Feb;16(2):365-375. 5. Tanaka S, et al. Protective Effects of Imatinib on Ischemia/Reperfusion Injury in Rat Lung. Ann Thorac Surg. 2016 Nov;102(5):1717-1724. 6. Maj E, et al. Vitamin D Analogs Potentiate the Antitumor Effect of Imatinib Mesylate in a Human A549 Lung Tumor Model. Int J Mol Sci. 2015 Nov 13;16(11):27191-207. 7. Zhao Q, Xing F, Tao Y, et al. Xiaozhang Tie Improves Intestinal Motility in Rats With Cirrhotic Ascites by Regulating the Stem Cell Factor/c-kit Pathway in Interstitial Cells of Cajal[J]. Frontiers in Pharmacology. 2020, 11.

文献引用

1. Zhao Q, Xing F, Tao Y, et al. Xiaozhang Tie Imp+J559:L621roves Intestinal Motility in Rats With Cirrhotic Ascites by Regulating the Stem Cell Factor/c-kit Pathway in Interstitial Cells of Cajal. Frontiers in Pharmacology. 2020, 11 2. Zhao Q, Xing F, Tao Y, et al. Xiaozhang Tie Improves Intestinal Motility in Rats With Cirrhotic Ascites by Regulating the Stem Cell Factor/c-kit Pathway in Interstitial Cells of Cajal. Frontiers in Pharmacology. 2020, 11.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

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

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Imatinib Mesylate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords