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Imatinib Mesylate

Catalog No. T1621   CAS 220127-57-1
Synonyms: ST-1571 Mesylate, PDGFR, Imatinib Mesylate, inhibit, CGP-57148B, Bcr-Abl, CD117, c-Kit, Platelet-derived growth factor receptor, STI 571, Inhibitor, SCFR, STI-571, Autophagy, Imatinib, STI571

Imatinib mesylate 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).

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Imatinib Mesylate, CAS 220127-57-1
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Imatinib mesylate 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).
Targets&IC50 c-Kit:0.1 μM, PDGFR:0.3 μM
In vitro 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].
In vivo 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].
Cell Research 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].
Animal Research 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].
Synonyms ST-1571 Mesylate, PDGFR, Imatinib Mesylate, inhibit, CGP-57148B, Bcr-Abl, CD117, c-Kit, Platelet-derived growth factor receptor, STI 571, Inhibitor, SCFR, STI-571, Autophagy, Imatinib, STI571
Molecular Weight 589.72
Formula C30H35N7O4S
CAS No. 220127-57-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 59 mg/mL (100 mM)

DMSO: 59 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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 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 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. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Autophagy Compound Library Cytokine Inhibitor Library TGF-beta/Smad Compound Library Hematonosis Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library

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