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| | N-Desmethyl Imatinib Basic information |
| | N-Desmethyl Imatinib Chemical Properties |
| Melting point | 99-101°C | | density | 1.268±0.06 g/cm3(Predicted) | | storage temp. | -20°C Freezer | | solubility | DMF: 16 mg/ml; DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml; DMSO: 14 mg/ml; Ethanol: 0.20 mg/ml | | form | A lyophilized solid | | pka | 13.28±0.70(Predicted) | | color | Light yellow to yellow | | biological source | synthetic | | InChIKey | BQQYXPHRXIZMDM-UHFFFAOYSA-N | | SMILES | C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)(=O)C1=CC=C(CN2CCNCC2)C=C1 |
| Safety Statements | 24/25 | | WGK Germany | WGK 3 | | HS Code | 29339900 | | Storage Class | 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | | Hazard Classifications | Carc. 2
Lact.
Muta. 2
Repr. 1B |
| | N-Desmethyl Imatinib Usage And Synthesis |
| Description | N-desmethyl Imatinib is a major active metabolite of imatinib , an anticancer agent that selectively targets tyrosine kinases, including Bcr-ABL, platelet-derived growth factor receptor (PDGFR), and KIT. N-desmethyl Imatinib is formed when imatinib undergoes demethylation by the cytochrome P450 (CYP) isomer CYP3A4. 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. | | Chemical Properties | Off-White to Pale-Yellow Solid | | Uses | aminoglycoside antibiotic similar to gentamycin, toxic to bacterial, yeast, higher plant and mammalian cells and to protozoans and helminthes | | Uses | anti-epileptic | | Uses | N-Desmethyl Imatinib (Imatinib EP Impurity C) is a metabolite of Gleevec, a tyrosine kinase inhibitor which is highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). It is a COVID19-related research product. | | Definition | ChEBI: N-Demethylated piperazine is a member of benzamides. | | References | [1] DRUKER B J. Translation of the Philadelphia chromosome into therapy for CML.[J]. Blood, 2008: 4808-4817. DOI: 10.1182/blood-2008-07-077958
[2] MüLLER B A. Imatinib and its successors–how modern chemistry has changed drug development.[J]. Current pharmaceutical design, 2009, 15 2: 120-133. DOI: 10.2174/138161209787002933
[3] OBACH R S. Pharmacologically active drug metabolites: impact on drug discovery and pharmacotherapy.[J]. Pharmacological Reviews, 2013, 65 2: 578-640. DOI: 10.1124/pr.111.005439 |
| | N-Desmethyl Imatinib Preparation Products And Raw materials |
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