General description
O-Desmethyl Gefitinib, a key metabolite of the anticancer drug gefitinib, belongs to the quinazoline family and is present in human plasma. Its formation is facilitated by the cytochrome P450 isoform CYP2D6. This compound exhibits significant activity as an inhibitor of tyrosine residue phosphorylation in EGFR, with an IC50 of 36 nM in subcellular assays. While its effectiveness is comparable to that of gefitinib, O-Desmethyl Gefitinib shows slightly reduced activity in whole-cell assays, with an IC50 of 760, in contrast to gefitinib′s 49 nM. Studies conducted in LoVo tumor mouse xenograft models have revealed that the tumor concentration of O-Desmethyl Gefitinib is notably lower than that of gefitinib, without causing a substantial reduction in tumor growth. Remarkably, increased plasma concentrations of O-Desmethyl Gefitinib in individuals homozygous for CYP2D6 do not lead to an increase in adverse effects. O-Desmethyl Gefitinib holds promise for biochemical and biomedical research, providing potential insights into drug development and cancer treatment.
Application
O-Desmethyl Gefitinib finds application in metabolomics and drug discovery research, particularly in the investigation of cancer and tumor management.
Biochem/physiol Actions
O-Desmethyl gefitinib is generated by the removal of a methyl group from gefitinib during the body′s metabolic processing of this compound within the body.
Features and Benefits
- High quality compound suitable for multiple research applications
- Compatible with a wide variety of chromatographic and spectrometry techniques
Other Notes
This product is intended for research purposes only, and it is not meant for human consumption.
- UPC:
- 51112004
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- SMB00950-5MG
- CAS:
- 847949-49-9
