O-Desmethyl gefitinib
Code | Size | Price |
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TAR-T16369-1mg | 1mg | £111.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Quantity:
TAR-T16369-5mg | 5mg | £161.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Quantity:
TAR-T16369-1mL | 1 mL * 10 mM (in DMSO) | £169.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T16369-10mg | 10mg | £214.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T16369-25mg | 25mg | £360.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T16369-50mg | 50mg | £533.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T16369-100mg | 100mg | £733.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C
Images
Documents
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.