O-Desmethyl gefitinib-d6

O-Desmethyl gefitinib-d6

• UNSPSC Description: O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. 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].
• Target Antigen: EGFR; Isotope-Labeled Compounds
• Type: Isotope-Labeled Compounds
• Related Pathways: JAK/STAT Signaling;Others;Protein Tyrosine Kinase/RTK
• Field of Research: Cancer
• Solubility: 10 mM in DMSO
• Smiles: OC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OC([2H])([2H])C([2H])([2H])C([2H])([2H])N4CCOCC4
• Molecular Weight: 438.91
• References & Citations: [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]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.|[3]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.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported