AG 213

Description

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. AG-213 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC₅₀ value of 2.4 μM in the human epidermoid carcinoma cell line A431.

The Uses of AG 213

Tyrphostin 47 is a potent inhibitor of EGFR kinase activity.

What are the applications of Application

Tyrphostin 47 is a potent inhibitor of EGFR kinase activity

Definition

ChEBI: 3-amino-2-[(3-hydroxy-4-oxo-1-cyclohexa-2,5-dienylidene)methyl]-3-mercapto-2-propenenitrile is a member of quinomethanes.

Biological Activity

Epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR) kinase inhibitor (IC 50 values are 2.4 and 3 μ M respectively). Stimulates microtubule polymerization and promotes neurite outgrowth > 17-fold over basal conditions in vitro . Also weakly inhibits protein kinase C (IC 50 = 60 μ M).

References

[1] romer l h, mclean n, turner c e, et al. tyrosine kinase activity, cytoskeletal organization, and motility in human vascular endothelial cells[j]. molecular biology of the cell, 1994, 5(3): 349-361.
[2] gazit a, yaish p, gilon c, et al. tyrphostins i: synthesis and biological activity of protein tyrosine kinase inhibitors[j]. journal of medicinal chemistry, 1989, 32(10): 2344-2352.
[3] levitzki a, gazit a. tyrosine kinase inhibition: an approach to drug development[j]. science, 1995, 267(5205): 1782.
[4] herbst r s. review of epidermal growth factor receptor biology[j]. international journal of radiation oncology biology physics, 2004, 59(2): s21-s26.