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O-Desmethyl gefitinib-d8

$480$1,300

Products Details

Product Description

– O-Desmethyl gefitinib-d8 is a 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].

Web ID

– HY-100064S

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C21H14D8ClFN4O3

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.

Molecular Weight

– 440.93

Compound Purity

– 99.84

SMILES

– OC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4C([2H])([2H])C([2H])([2H])OC([2H])([2H])C4([2H])[2H]

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– 10 mM in DMSO

Target

– EGFR

Pathway

– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

Product type

– Isotope-Labeled Compounds

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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