2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-

Описание

Overactivity of epidermal growth factor receptor (EGFR) tyrosine kinase activity has been associated with a number of cancers. CL 387,785 is a potent, irreversible inhibitor of EGFR kinase activity (IC₅₀ = 370 pM). It blocks EGF-stimulated autophosphorylation of receptors in cells (IC₅₀ = 5 nM) and halts cell cycling in cells that overexpress EGFR or c-ErbB2 (IC₅₀s = 31-125 nM). CL 387,785 profoundly blocks the growth of EGFR-overexpressing tumors in nude mice when given orally at 80 mg/kg/day for 10 days.

Использование

CL-387785 (EKI-785) is an irreversible and selective EGFR inhibitor showing activity against mutations of the receptor. Potential therapeutic against various type of cancer, including lung cancer.

Определение

ChEBI: A member of the class of quinazolines that is 4,6-diaminoquinazoine in which the one of the hydrogens attached to the amino group at position 4 has been replaced by a m-bromophenyl group while one of the hydrogens attached to the amino group a position 6 has been replaced by a but-2-ynoyl group.