Description
PD153035 can inhibit epidermal growth factor (EGF) receptor tyrosine kinase with Ki of 6 pM.
Storage
2 years at -20 centigrade
Molecular Formula
C16H14BrN3O2.HCl
Chemical Name
N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride
Solubility
DSMO 0.5 mg/mL Water
In vitro
PD153035 can inhibit epidermal growth factor (EGF) receptor tyrosine kinase with Ki of 6 pM. PD153035 can potently suppresses tyrosine phosphorylation of the EGF receptor in A431 cells at nanomolar concentrations. PD153035 inhibits EGF-dependent EGF receptor phosphorylation and suppresses the proliferation and clonogenicity of a wide panel of EGF receptor-overexpressing human cancer cell lines. EGF receptor autophosphorylation in response to exogenous EGF was completely inhibited at PD153035 concentrations of >75 nM in cells overexpressing the EGF receptor.
In vivo
In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035(80 mg/kg) suppresse the tyrosine phosphorylation of the EGF receptor rapidly by 80-90% in the tumors.
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