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OSI-420 free base

In stock
Catalog No.
B1495
EGFR inhibitor
Grouped product items
SizePriceStock Qty
5mg
$119.00
In stock
10mg
$225.00
In stock
50mg
$539.00
In stock

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Background

OSI-420 is the major metabolite of OSI-774(erlotinib) which is a small molecule, orally active, potent, and selective inhibitor of EGFR tyrosine kinase with an IC50 value of 2nM[1,2].

OSI-420 is the active metabolite of OSI-774(erlotinib) which selectively inhibits the EGFR tyrosine kinase and prevents autophosphorylation by competing with adenosine triphosphate (ATP) for its binding site on the intracellular domain of EGFR. In addition, erlotinib, is metabolized to produce ATP, has been found to be selective for EGFR and lead to the induction of apoptosis by inducing the disruption of mitochondrial effect on loss of mitochondrial membrane potential and release of cytocrome c [1, 2].

References:
[1] Zhang W1, Siu LL, Moore MJ, Chen EX.Simultaneous determination of OSI-774 and its major metabolite OSI-420 in human plasma by using HPLC with UV detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Jan 5;814(1):143-7.
[2] Bonomi P. Erlotinib: a new therapeutic approach for non-small cell lung cancer.Expert Opin Investig Drugs. 2003 Aug;12(8):1395-401.

Chemical Properties

StorageStore at -20°C
M.Wt379.41
Cas No.183320-51-6
FormulaC21H21N3O4
SynonymsOSI-420, Desmethyl Erlotinib, CP-473420
SolubilitySoluble in DMSO
Chemical Name2-((4-((3-ethynylphenyl)amino)-7-(2-methoxyethoxy)quinazolin-6-yl)oxy)ethanol
SDFDownload SDF
Canonical SMILESC#CC1=CC(NC2=NC=NC3=C2C=C(OCCO)C(OCCOC)=C3)=CC=C1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
Targets EGFR          
IC50            

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