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
CAS Number
[847949-49-9]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/o-desmethyl-gefitinib.html
Concentration
10mM
Purity
99.40
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
OC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4CCOCC4
Molecular Formula
C21H22ClFN4O3
Molecular Weight
432.88
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Curated Selection
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