AG 213 Property

Melting point:

213 °C

Boiling point:

474.5±55.0 °C(Predicted)

Density 

1.512±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 50 mg/mL, clear, orange

form 

Orange solid.

pka

8.82±0.10(Predicted)

Safety

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

3

F 

10

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

AG 213 Chemical Properties,Usage,Production

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.

Uses

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.