TargetMol

O-Desmethyl gefitinib

Product Code:
 
TAR-T16369
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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CodeSizePrice
TAR-T16369-1mg1mg£111.00
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TAR-T16369-5mg5mg£161.00
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TAR-T16369-1mL1 mL * 10 mM (in DMSO)£169.00
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TAR-T16369-10mg10mg£214.00
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TAR-T16369-25mg25mg£360.00
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TAR-T16369-50mg50mg£533.00
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TAR-T16369-100mg100mg£733.00
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Further Information

Bioactivity:
O-Desmethyl gefitinib inhibits EGFR (IC50: 36 nM in subcellular assays). In human plasma, O-Desmethyl gefitinib is an active metabolite of Gefitinib. The formation of O-desmethyl gefitinib is dependent on the CYP2D6 activity.
CAS:
847949-49-9
Formula:
C21H22ClFN4O3
Molecular Weight:
432.88
Pathway:
Tyrosine Kinase/Adaptors|Angiogenesis|JAK/STAT signaling
Purity:
0.996
SMILES:
Oc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCN1CCOCC1
Target:
EGFR

References

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. 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.