GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Gleevec, Glivec, CGP057148B | 4-​[(4-​methyl-​1-​piperazinyl)​methyl]​-​N-​[4-​methyl-​3-​[[4-​(3-​pyridinyl)​-​2-​pyrimidinyl]​amino]​phenyl]​-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor oftyrosine kinasewith inhibition forv-Abl,c-KitandPDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) inducesautophagy.
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%

Specifications

Synonyms

Gleevec, Glivec, CGP057148B | 4-​[(4-​methyl-​1-​piperazinyl)​methyl]​-​N-​[4-​methyl-​3-​[[4-​(3-​pyridinyl)​-​2-​pyrimidinyl]​amino]​phenyl]​-benzamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophag

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of ABL proto-oncogene 1; non-receptor tyrosine kinase;Inhibitor of discoidin domain receptor tyrosine kinase 1;Inhibitor of discoidin domain receptor tyrosine kinase 2

Names and Identifiers

• 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
• Molecular Weight: 493.6
• Reaxy-Rn: 7671333
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7671333&ln=

Associated Targets(Human)

DDR2 Tchem Discoidin domain-containing receptor 2 (3 Activities)

Discover Target: DDR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (3 Activities)

Discover Target: CSF1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DDX3X Tchem ATP-dependent RNA helicase DDX3X (1 Activities)

Discover Target: DDX3X

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DDR1 Tchem Epithelial discoidin domain-containing receptor 1 (5 Activities)

Discover Target: DDR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABCB1 Tchem Multidrug resistance protein 1 (1 Activities)

Discover Target: ABCB1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC47A2 Tchem Multidrug and toxin extrusion protein 2 (1 Activities)

Discover Target: SLC47A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC47A1 Tchem Multidrug and toxin extrusion protein 1 (3 Activities)

Discover Target: SLC47A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter (1 Activities)

Discover Target: SLC6A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TBXAS1 Tchem Thromboxane-A synthase (1 Activities)

Discover Target: TBXAS1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha (3 Activities)

Discover Target: PDGFRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRB Tclin Platelet-derived growth factor receptor beta (3 Activities)

Discover Target: PDGFRB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA6 Tclin Carbonic anhydrase 6 (1 Activities)

Discover Target: CA6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA1 Tclin Carbonic anhydrase 1 (1 Activities)

Discover Target: CA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA3 Tclin Carbonic anhydrase 3 (1 Activities)

Discover Target: CA3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA2 Tclin Carbonic anhydrase 2 (1 Activities)

Discover Target: CA2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA12 Tclin Carbonic anhydrase 12 (1 Activities)

Discover Target: CA12

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA14 Tclin Carbonic anhydrase 14 (1 Activities)

Discover Target: CA14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA9 Tclin Carbonic anhydrase 9 (1 Activities)

Discover Target: CA9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA7 Tclin Carbonic anhydrase 7 (1 Activities)

Discover Target: CA7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCR Tclin Breakpoint cluster region protein (1 Activities)

Discover Target: BCR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABCG2 Tchem ATP-binding cassette sub-family G member 2 (2 Activities)

Discover Target: ABCG2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL2 Tchem Tyrosine-protein kinase ABL2 (6 Activities)

Discover Target: ABL2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 (19 Activities)

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit (10 Activities)

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NQO2 Tchem Ribosyldihydronicotinamide dehydrogenase [quinone] (5 Activities)

Discover Target: NQO2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 47 mg/mL (198.92 mM); Ethanol: 18 mg/mL (76.18 mM); Water: Insoluble
• Refractive Index: 1.67
• Boil Point(°C): 715.75° C
• Melt Point(°C): 211-213°C

References

1. Yao Liu, Zhichao He, Heng Liang, Minzhen Han, Jinxingyi Wang, Qian Liu, Yanping Guan.  (2023)  A high-throughput UHPLC-MS/MS method for the determination of eight anti-tumor drugs in plasma.  ANALYTICAL BIOCHEMISTRY,      [PMID:37429484] [10.1016/j.ab.2023.115230]

2. Fangjun Chen, Wenda Chen, Zhenxin Wang, Yingfei Peng, Beili Wang, Baishen Pan, Wei Guo.  (2023)  Development and clinical application of a liquid chromatography-tandem mass spectrometry-based assay to quantify eight tyrosine kinase inhibitors in human plasma.  Journal of Mass Spectrometry and Advances in the Clinical Lab,      [PMID:37234251] [10.1016/j.jmsacl.2023.05.001]

3. Siyu Wang, Lutong Wang, Jingwen Xu, Yihai Wang, Limin Xiang, Xiangjiu He.  (2023)  Synergistic Combination of the Total Steroidal Saponins from the Berries of Black Nightshade and Adriamycin to Overcome Leukemia Multidrug Resistance.  JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,      [PMID:36752041] [10.1021/acs.jafc.2c07740]

4. 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).  [PMID:] [10.1007/s10118-022-2726-0]

5. Shengmei Wang, Xuanjun Liu, Shengfeng Wang, Linqi Ouyang, Hui Li, Jinsong Ding, Guiming Deng, Wenhu Zhou.  (2021)  Imatinib co-loaded targeted realgar nanocrystal for synergistic therapy of chronic myeloid leukemia.  JOURNAL OF CONTROLLED RELEASE,      [PMID:34428479] [10.1016/j.jconrel.2021.08.035]

6. Hao Gu, Kang Ma, Weiqian Zhao, Lirong Qiu, Wei Xu.  (2021)  A general purpose MALDI matrix for the analyses of small organic, peptide and protein molecules.  ANALYST,  146  (12): (4080-4086).  [PMID:34052846] [10.1039/D1AN00474C]

7. Yao Yang, Zhengwei Huang, Jinyuan Li, Ziran Mo, Ying Huang, Cheng Ma, Wenhao Wang, Xin Pan, Chuanbin Wu.  (2019)  PLGA Porous Microspheres Dry Powders for Codelivery of Afatinib-Loaded Solid Lipid Nanoparticles and Paclitaxel: Novel Therapy for EGFR Tyrosine Kinase Inhibitors Resistant Nonsmall Cell Lung Cancer.  Advanced Healthcare Materials,  8  (23): (1900965).  [PMID:31664795] [10.1002/adhm.201900965]

8. Xinwei Liu, Xiao Wang, Jiexun Bu, Xiaoyu Zhou, Zheng Ouyang.  (2018)  Tandem Analysis by a Dual-Trap Miniature Mass Spectrometer.  ANALYTICAL CHEMISTRY,      [PMID:30444599] [10.1021/acs.analchem.8b03958]

9. Yanting Zhu, Fangwei Li, Wenhua Shi, Cui Zhai, Jian Wang, Xin Yan, Qingting Wang, Qianqian Zhang, Lan Yang, Li Gao, Manxiang Li.  (2018)  COP9 signalosome subunit 6 mediates PDGF -induced pulmonary arterial smooth muscle cells proliferation.  EXPERIMENTAL CELL RESEARCH,      [PMID:30180991] [10.1016/j.yexcr.2018.08.032]

10. Xiaoyu Zhou, Xinwei Liu, Spencer Chiang, Wenbo Cao, Ming Li, Zheng Ouyang.  (2018)  Stimulated Motion Suppression (STMS): a New Approach to Break the Resolution Barrier for Ion Trap Mass Spectrometry.  JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY,      [PMID:29845562] [10.1007/s13361-018-1995-x]

11. Rongrong Fu, Rui Chang, Andong Peng, Changshun Feng, Weifan Zhu, Yi Chen, Xue Tian, Rui Wang, Hui Yan, Dianlong Jia, Jun Li.  (2024)  Efficient treatment of colon cancer with codelivery of TRAIL and imatinib by liposomes.  PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY,      [PMID:38230653] [10.1080/10837450.2024.2301763]

12. Feng Jingting, Jiang Yuhan, Liu Sihan, Deng Linge, Lv Yanni, Chen Nanzheng, Han Shengli.  (2024)  KIT-SNAP-tag/cell membrane chromatography model coupled with liquid chromatography–mass spectrometry for anti-GIST compound screening from Evodia rutaecarpa.  ANALYTICAL AND BIOANALYTICAL CHEMISTRY,      [PMID:38231254] [10.1007/s00216-024-05148-5]

13. Pengfei Ding, Zhuyun Liu, YuQi Wu, Chunyan Zong, Yuming Wang, Yushan Xu, Kaijun Xu, Lizhong Wang.  (2025)  Preparation, structure characterization and solubility of one cocrystal and one salt of Imatinib with Citric acid and Fumaric acid.  JOURNAL OF MOLECULAR STRUCTURE,      [PMID:] [10.1016/j.molstruc.2025.141769]

14. Ninghong Li, Lu Liu, Dong Liu, Hengyi Yu, Guangjie Yang, Lihui Qiu, Yufei Chen, Dong Xiang, Xuepeng Gong.  (2024)  Simultaneous determination of three tyrosine kinase inhibitors and three triazoles in human plasma by LC-MS/MS: applications to therapeutic drug monitoring and drug-drug interaction studies.  JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,      [PMID:39208604] [10.1016/j.jchromb.2024.124276]

15. Xiaoqian Jiang, Aihua Qu, Xinxin Xu, Hua Kuang, Liqiang Liu, Chuanlai Xu.  (2024)  Ultrasensitive detection of imatinib in human serum using a gold-based paper sensor.  JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,      [PMID:38281369] [10.1016/j.jchromb.2024.124001]