N-Desmethyl imatinib mesylate
Based on 1 publication(s) in Google Scholar
N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.
For research use only. We do not sell to patients.
- CAS No.: 404844-03-7
- Formula: C29H33N7O4S
- Molecular Weight:575.68
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Storage:
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) N-Desmethyl imatinib mesylate
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
1558 nM
Compound: 2, CGP74588
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Inhibition of human BCR-ABL1 expressed in mouse BA/F3 cells assessed as cell growth inhibition by ATP-depletion assay
Inhibition of human BCR-ABL1 expressed in mouse BA/F3 cells assessed as cell growth inhibition by ATP-depletion assay
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[PMID: 23611771] |
| BaF3 | IC50 |
2229 nM
Compound: 2, CGP74588
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Inhibition of human BCR-ABL1 autophosphorylation expressed in mouse BA/F3 cells by ELISA
Inhibition of human BCR-ABL1 autophosphorylation expressed in mouse BA/F3 cells by ELISA
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[PMID: 23611771] |
N-Desmethyl imatinib (CGP 74588) (0.3-30 μM) mesylate acts as a substrate for P-glycoprotein, stimulating ATPase activity in P-glycoprotein-expressing Sf9 cell membrane vesicles at concentrations ranging from 0.3 to 30 μM[3].
N-Desmethyl imatinib (48 h) mesylate inhibits K562 cell proliferation with an IC50 of 0.58 μM and shows no significant inhibition of K562/Dox cell proliferation (IC50 > 20 μM) after 48 h of treatment[3].
N-Desmethyl imatinib (1.6 μM, 20 μM; 48 h) mesylate induces apoptosis in K562 cells, but does not significantly induce apoptosis in K562/Dox cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 404844-03-7
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Molecular Weight 575.68
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Formula C29H33N7O4S
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SMILES
CS(=O)(O)=O.O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CC=N2)=C1)C4=CC=C(CN5CCNCC5)C=C4
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Synonyms
Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate; CGP 74588 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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J Chromatogr B Analyt Technol Biomed Life Sci
Imatinib and norimatinib therapeutic monitoring using dried blood spots: Analytical and clinical validation, and performance comparison of volumetric collection devices. [Abstract]2025 Apr 1:1255:124526. PMID: 39985852
Purity & Documentation
References
[1]. Rymbai E, et al. The identification of c-Abl inhibitors as potential agents for Parkinson's disease: a preliminary in silico approach. Mol Divers. 2024;28(6):4051-4065. [Content Brief]
[2]. Gagno S, et al. Increased plasma imatinib exposure and toxicity in chronically treated GIST patients with SARS-CoV-2 infection: a case series. Front Immunol. 2024;15:1441620. Published 2024 Oct 9. [Content Brief]
[3]. Mlejnek P, et al. Interactions of N-desmethyl imatinib, an active metabolite of imatinib, with P-glycoprotein in human leukemia cells. Ann Hematol. 2011;90(7):837-842. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
N-Desmethyl imatinib mesylate Related Classifications
HY-G0017A Related Classifications
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