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O-Desmethyl gefitinib
SKU
HY-100064-10 mg
Category Reference compound
Tags Cancer, EGFR, JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
$150 – $780
Products Details
Product Description
– 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].
Web ID
– HY-100064
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular 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
Compound Purity
– 99.40
SMILES
– OC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4CCOCC4
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 100 mg/mL (ultrasonic)
Target
– EGFR
Pathway
– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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