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Formula | C29H31N7O |
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Molecular Weight | 493.6 | CAS No. | 152459-95-5 | ||||
Solubility (25°C)* | In vitro | DMSO | 25 mg/mL (50.64 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Imatinib 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 autophagy. | ||||||
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Targets |
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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. [1] 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. [2] 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. [3] 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. [4] |
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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. [5] 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. [6] |
Kinase Assay: |
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Cell Assay: |
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Data from [Leukemia Res, 2012, 36, 1311-1314]
Data from [FASEB J, 2011, 25, 3661-3673]
, , Dr. Thomas Kruwel of Fraunhofer
, , Dr. Helen Rizos from the university of Sydney
Genome-wide Cas9-mediated screening of essential non-coding regulatory elements via libraries of paired single-guide RNAs [ Nat Biomed Eng, 2024, 10.1038/s41551-024-01204-8] | PubMed: 38778183 |
Targeting PDGF signaling of cancer-associated fibroblasts blocks feedback activation of HIF-1α and tumor progression of clear cell ovarian cancer [ Cell Rep Med, 2024, S2666-3791(24)00201-5] | PubMed: 38670097 |
The molecular basis of Abelson kinase regulation by its αI-helix [ Elife, 2024, 12RP92324] | PubMed: 38588001 |
Cancer-Associated Fibroblasts Promote Lymphatic Metastasis in Cholangiocarcinoma via the PDGF-BB/PDGFR-β Mediated Paracrine Signaling Network [ Aging Dis, 2024, 15(1):369-389] | PubMed: 37307823 |
Cancer-Associated Fibroblasts Promote Lymphatic Metastasis in Cholangiocarcinoma via the PDGF-BB/PDGFR-β Mediated Paracrine Signaling Network [ Aging Dis, 2024, 15(1):369-389] | PubMed: 37307823 |
Regulation of Cell Cycle Progression through RB Phosphorylation by Nilotinib and AT-9283 in Human Melanoma A375P Cells [ Int J Mol Sci, 2024, 25(5)2956] | PubMed: 38474202 |
Asciminib Maintains Antibody-Dependent Cellular Cytotoxicity against Leukemic Blasts [ Cancers (Basel), 2024, 16(7)1288] | PubMed: 38610966 |
Neratinib plus dasatinib is highly synergistic in HER2-positive breast cancer in vitro and in vivo [ Transl Oncol, 2024, 49:102073] | PubMed: 39191139 |
Arbutus unedo L. Fractions Exhibit Chemotherapeutic Properties for the Treatment of Gastrointestinal Stromal Tumors [ Plants (Basel), 2024, 13(9)1201] | PubMed: 38732416 |
CFL1 is Implicated in Chronic Myeloid Leukemia Response during Imatinib Therapy [ J Cancer, 2024, 15(8):2424-2430] | PubMed: 38495482 |
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