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%
| 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 |
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| WGK Germany | 3 |
| Molecular Weight | 589.71 |
| Reaxy-Rn | 10229624 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10229624&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubility | 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); |
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| 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, [PMID:] [10.1016/j.microc.2026.116962] |
