A major active metabolite of imatinib; formed through demethylation of imatinib by CYP3A4; has the same in vitro potency at Bcr-ABL kinase as imatinib (IC50 = 38 nM for both) but is only present in plasma at 10-15% of the levels of imatinib

N-Desmethyl Imatinib – 500 µg

Brand:
Cayman
CAS:
404844-02-6
Storage:
-20
UN-No:
Non-Hazardous - /

N-desmethyl Imatinib is a major active metabolite of imatinib (Item No. 13139), an anticancer agent that selectively targets tyrosine kinases, including Bcr-ABL, platelet-derived growth factor receptor (PDGFR), and KIT.{17064,17065} N-desmethyl Imatinib is formed when imatinib undergoes demethylation by the cytochrome P450 (CYP) isomer CYP3A4.{40229} N-desmethyl Imatinib has the same in vitro potency at Bcr-ABL kinase as imatinib (IC50 = 38 nM for both) but is only present in plasma at 10-15% of the levels of imatinib, indicating the majority of the anticancer activity can be attributed to the parent compound.  

 

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Description

A major active metabolite of imatinib; formed through demethylation of imatinib by CYP3A4; has the same in vitro potency at Bcr-ABL kinase as imatinib (IC50 = 38 nM for both) but is only present in plasma at 10-15% of the levels of imatinib

Formal name: N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-4-(1-piperazinylmethyl)-benzamide

Synonyms:  N-Desmethyl Gleevec|STI-509-00

Molecular weight: 479.6

CAS: 404844-02-6

Purity: ≥95%

Formulation: A lyophilized solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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