404844-03-7
Chemical Structure
N-Desmethyl imatinib mesylate
Synonym(s): Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate; CGP 74588 mesylate
- CAS No.: 404844-03-7
- Formula:C29H33N7O4S
- Molecular Weight:575.68
IUPAC Name: N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(piperazin-1-ylmethyl)benzamide methanesulfonate
InChIKey: BRTOZFXRYMYSOF-UHFFFAOYSA-N
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
Biological Activity: 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[1][2][3].
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N-Desmethyl imatinib mesylate | 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. | |||||||||||||||||||||
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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]
