4-[(3-BROMOPHENYL)AMINO]-6-PROPIONYLAMIDOQUINAZOLINE

Description

PD 174265 is a potent, cell-permeable inhibitor of the tyrosine kinase activity of the epidermal growth factor (EGF) receptor (IC₅₀ = 0.45 nM). It is effective in cells, blocking tyrosine phosphorylation induced by either EGF or heregulin (IC₅₀s = 39 and 220 nM, respectively). The action of PD 174265 is reversible, which makes it a useful tool for comparative studies with irreversible inhibitors of EGFR kinase activity.

Uses

PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR tyrosine kinase activity.

General Description

A potent, cell-permeable, reversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC₅₀ = 450 pM). The reversible nature of this compound makes it a less effective antitumor agent than PD 168393 (Cat. No. 513033).

Biochem/physiol Actions

Target IC50: 450 pM against EGF receptor (EGFR) tyrosine kinase activity

Enzyme inhibitor

This substituted quinazoline (FWfree-base = 371.24 g/mol), also known as 4- [(3-bromophenyl)amino]-6-propionylamidoquinazoline, inhibits epidermal growth factor receptor (EGFR) protein-tyrosine kinase, IC50 = 0.45 nM. PD 174265 selectively targets and irreversibly inactivates the epidermal growth factor receptor tyrosine kinase through specific, covalent modification of a Cys-773. See also PD 168393