Imatinib Mesylate (STI571)是Imatinib的甲磺酸盐，具有较好的口服生物利用度，是一种多靶点的抑制剂，同时作用于v-Abl， c-Kit和PDGFR，IC50分别为0.6 μM， 0.1 μM 和0.1 μM。A c-Abl, PDGFR, and c-kit inhibitor

Information

Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor ofv-Abl,c-KitandPDGFRwithIC50of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib M
In vitro

In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis.

In vivo

Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation.
Cell Data

cell lines：

Concentrations：~100 μM

Incubation Time：48 hours

Powder Purity:≥99%

规格

英文别名

Gleevec, Glivec, CGP-57148B | N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonic acid

规格或纯度

10mM in DMSO

英文名称

Imatinib (STI571) Mesylate

生化机理

甲磺酸伊马替尼（STI571，CGP057148B，格列卫）是伊马替尼的口服生物利用度甲磺酸盐，是v-Abl、c-Kit和PDGFR的多靶点抑制剂，在无细胞或基于细胞的试验中，IC50分别为0.6 μM、0.1 μM和0.1 μM。甲磺酸伊马替尼（STI571）诱导自噬。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

作用机制

干细胞生长因子受体抑制剂

名称和识别符

EC号

606-892-3

分子类型

小分子

Isomeric 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

分子量

589.71

Reaxy-Rn

10229624

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10229624&ln=

技术文档

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高级数据

化学和物理性质

溶解性

Solubility (25°C) In vitro DMSO: 47 mg/mL (198.89 mM); Ethanol: 47 mg/mL (198.89 mM); Water: 15 mg/mL (63.47 mM);

安全和危险性（GHS）

象形图

GHS08, GHS07

信号词

Danger

危险声明

H351: 怀疑引起遗传缺陷

H302: 吞食有害

H360: 可能损害生育力或未出生的孩子

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P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P270: 使用本产品时，请勿进食、饮水或吸烟。

P330: 漱口

P203: 使用前，获取、阅读并遵守所有安全说明。

P301+P317: 如果被吞咽：请寻求医疗帮助。

P318: 如果暴露或担心，请就医。

WGK Germany

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

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技术文档和文章

小分子抑制剂科研选型指南：最小证据链与场景化验证框架（含选型矩阵、案例卡片与产品表1–表4）

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Small-Molecule Inhibitors: A Practical Guide for Research Selection — A Minimal Evidence Chain and Scenario-Based Validation Framework (Including a Selection Matrix, Case Cards, and Product Tables 1–4)

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Small-Molecule Inhibitors

蛋白酪氨酸激酶/RTK信号转导机制与疾病研究

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EGFR JAK FGFR VEGFR 蛋白酪氨酸激酶 RTK NRTK Src Abl 肿瘤靶向治疗

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MAPK/ERK 信号通路：RAS–RAF–MEK–ERK 级联调控、细胞功能输出与研究工具应用

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MAPK/ERK Signaling Pathway: RAS–RAF–MEK–ERK Cascade Regulation, Cellular Functional Outputs, and Research Tool Applications

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此产品的引用文献

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引用文献

1. Ju Huang, Jian Chen. (2023) Pharmacokinetics and pharmacodynamic evaluation of hyaluronic acid-modified imatinib-loaded PEGylated liposomes in CD44-positive Gist882 tumor-bearing mice. JOURNAL OF LIPOSOME RESEARCH, [PMID:37401372] [10.1080/08982104.2023.2228888]
2. Chengzhu Song, Dongning Li, Jie Zhang, Xiaoyan Zhao. (2023) Berberine hydrochloride alleviates imatinib mesylate – induced cardiotoxicity through the inhibition of Nrf2-dependent ferroptosis. Food & Function, 14 (2): (1087-1098). [PMID:36594456] [10.1039/D2FO03331C]
3. Wang Cong-Yu, Sun Min, Fan Zhen, Du Jian-Zhong. (2022) Intestine Enzyme-responsive Polysaccharide-based Hydrogel to Open Epithelial Tight Junctions for Oral Delivery of Imatinib against Colon Cancer. CHINESE JOURNAL OF POLYMER SCIENCE, 40 (10): (1154-1164). [10.1007/s10118-022-2726-0]
4. Yang Li, Xiaoyan Liu, Zhongming Liu, Shoujuan Wang, Fangong Kong. (2025) Fabrication of controllable structure of nanocellulose composite aerogel for targeted drug delivery. CARBOHYDRATE POLYMERS, [PMID:40383578] [10.1016/j.carbpol.2025.123518]
5. Xiaorui Shi, Chong Hu, Liangli Fan, Bin Guo, Jingyu Zhang, Chu Tang, Fu Wang. (2024) High-Throughput Computer Screen Aids Discovery of Methotrexate as miR-20b Inhibitor to Suppress Nonsmall Cell Lung Cancer Progression. ACS Chemical Biology, [PMID:39736132] [10.1021/acschembio.4c00706]
6. Sai-Nan Qin, Yi-Xue Zhang, Yi-Jie Cao, Ting Wan, Yi-Yang Zhou, Shan-Shan Su, Yu-Qiong Guo, Jian-Jun Sun, Kalle Salminen. (2026) A self-assembled electrochemical aptasensor for one-step rapid detection of cisplatin in blood via aptamer conformational change. MICROCHEMICAL JOURNAL, [10.1016/j.microc.2026.116962]
7. Yuanyuan Liu, Yuanyao Lin, Xuemei He. (2026) Ultrasound-responsive PLGA nanoparticles co-loaded with celecoxib and catalase enhance the therapeutic efficacy of imatinib in gastrointestinal stromal tumors. INTERNATIONAL JOURNAL OF PHARMACEUTICS, [10.1016/j.ijpharm.2026.127320]