Product Description: O-Desmethyl gefitinib (Standard) is the analytical standard of O-Desmethyl gefitinib. This product is intended for research and analytical applications. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
Formula: C21H22ClFN4O3
References: [1]Kobayashi H, et al. Effects of polymorphisms in CYP2D6 and ABC transporters and side effects induced by gefitinib on the pharmacokinetics of the gefitinib metabolite, O-desmethyl gefitinib. Med Oncol. 2016 Jun;33(6):57./[2]McKillop D, et al. Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition. Xenobiotica. 2006 Jan;36(1):29-39.
CAS Number: 847949-49-9
Molecular Weight: 432.88
Research Area: Cancer
Target: EGFR;Reference Standards
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