O-Desmethyl gefitinib-d6
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].
Product Specifications
UNSPSC
12352005
Target
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 Formula
C21H16D6ClFN4O3
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
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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