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Imatinib Mesylate

Catalog No. T1621   CAS 220127-57-1
Synonyms: ST-1571 Mesylate, STI-571, CGP-57148B

Imatinib Mesylate (STI-571) 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 Chemical Structure
Imatinib Mesylate, CAS 220127-57-1
Pack Size Availability Price/USD Quantity
200 mg In stock $ 54.00
500 mg In stock $ 82.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 100%
Purity: 99.73%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Imatinib Mesylate (STI-571) 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, STI-571, CGP-57148B
Molecular Weight 589.71
Formula C29H31N7O·CH4SO3
CAS No. 220127-57-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 59 mg/mL (100 mM)

DMSO: 59 mg/mL (100 mM)

TargetMolReferences and Literature

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 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.

TargetMolCitations

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 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library FDA-Approved Kinase Inhibitor Library Hematopoietic Toxicity Compound Library Bioactive Compound Library Targeted Therapy Drug Library Drug Repurposing Compound Library

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Keywords

Imatinib Mesylate 220127-57-1 Angiogenesis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl PDGFR c-Kit inhibit ST-1571 Mesylate STI 571 STI571 CD117 Platelet-derived growth factor receptor Inhibitor STI-571 ST1571 Mesylate SCFR ST 1571 Mesylate Imatinib CGP-57148B inhibitor

 

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