Description
As the major metabolite of Erlotinib, OSI-420 can inhibit EGFR with IC50 of 2 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C21H21N3O4.HCl
Chemical Name
2-(4-(3-ethynylphenylamino)-7-(2-methoxyethoxy)quinazolin-6-yloxy)ethanol hydrochloride
Solubility
DSMO 83 mg/mL Water 2 mg/ml Ethanol
In vitro
OSI-420 is the major metabolite of Erlotinib in human plasma. Erlotinib growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 uM.
In vivo
At doses of 100 mg/kg, Erlotinib completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice.
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