Search Site
Related Products
OSI-420EGFR inhibitor

OSI-420

Catalog No. B1495
Size Price Stock Qty
5mg $119.00 In stock
10mg $225.00 In stock
50mg $539.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

OSI-420

Biological Activity

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

OSI-420 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

OSI-420 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 183320-51-6 SDF Download SDF
Chemical Name 2-[4-(3-ethynylanilino)-7-(2-methoxyethoxy)quinazolin-6-yl]oxyethanol;hydrochloride
Canonical SMILES COCCOC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCO.Cl
Formula C21H22ClN3O4 M.Wt 415.87
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips N/A
Shipping Condition N/A

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.