CEP-751 inhibits TRK receptor tyrosine kinase activity in vitro exhibits anti-tumor activity.
Int J Cancer
; 72(4): 673-9, 1997 Aug 07.
Article
em En
| MEDLINE
| ID: mdl-9259409
The present report describes the in vitro and in vivo profile of CEP-751, a novel receptor tyrosine kinase inhibitor. CEP-751 at 100 nM inhibits the receptor tyrosine kinase activity of the neurotrophin receptors trkA, trkB and trkC. CEP-751 has no effect on activity of receptors for EGF, IGF-I, insulin or on erbB2; inhibition of receptors for PDGF and bFGF was observed but occurred with lesser potency than inhibition of trk. CEP-751 exhibited anti-tumor efficacy against tumors derived from NIH3T3 cells transfected with trkA. Inhibition of trk phosphorylation could also be measured in these tumors, suggesting that anti-tumor efficacy of CEP-751 is related to inhibition of trk receptor tyrosine kinase activity. CEP-751 was found to be without effect when administered to nude mice bearing SK-OV-3 tumors, which overexpress erbB2 receptors, providing further evidence that inhibition of tumor growth may be related to inhibition of trk receptor tyrosine kinase activity. Our data indicate that CEP-751 is a potent trk inhibitor which possesses anti-tumor activity.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Carbazóis
/
Proteínas Proto-Oncogênicas
/
Receptores de Fator de Crescimento Neural
/
Receptores Proteína Tirosina Quinases
/
Inibidores Enzimáticos
/
Antineoplásicos
Limite:
Animals
Idioma:
En
Revista:
Int J Cancer
Ano de publicação:
1997
Tipo de documento:
Article
País de afiliação:
Estados Unidos
País de publicação:
Estados Unidos