A major active metabolite of imatinib
Related Products
Parent Compound(s)
13139Imatinib (mesylate)
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N-desmethyl Imatinib

Item No. 16947

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-4-(1-piperazinylmethyl)-benzamide
CAS Number
404844-02-6
Synonyms
  • N-desmethyl Gleevec
  • STI-509-00
Molecular Formula
C28H29N7O
Formula Weight
479.6
Purity
≥95%
Formulation (Request formulation change)
A lyophilized solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMF:PBS (pH 7.2) (1:4): 0.20 mg/mlDMSO: 14 mg/mlEthanol: 0.20 mg/ml
λmax
237, 270 nm
SMILES
O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CC=N2)=C1)C(C=C4)=CC=C4CN5CCNCC5
InChi Code
InChI=1S/C28H29N7O/c1-20-4-9-24(17-26(20)34-28-31-12-10-25(33-28)23-3-2-11-30-18-23)32-27(36)22-7-5-21(6-8-22)19-35-15-13-29-14-16-35/h2-12,17-18,29H,13-16,19H2,1H3,(H,32,36)(H,31,33,34)
InChi Key
BQQYXPHRXIZMDM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Product Description

    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.1,2 N-desmethyl Imatinib is formed when imatinib undergoes demethylation by the cytochrome P450 (CYP) isomer CYP3A4.3 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Druker, B.J. Translation of the Philadelphia chromosome into therapy for CML. Blood 112(13), 4808-4817 (2008).

    2. Müller, B.A. Imatinib and its successors-how modern chemistry has changed drug development. Curr. Pharm. Des. 15(2), 120-133 (2009).

    3. Obach, R.S. Pharmacologically active drug metabolites: Impact on drug discovery and pharmacotherapy. Pharmacol. Rev. 65(2), 578-640 (2013).