AG 213

CAS NO.：122520-86-9
Empirical Formula: C10H8N2O2S
Molecular Weight: 220.25
MDL number: MFCD00133902
SAFETY DATA SHEET (SDS)
Update Date: 2023-05-18 11:31:21

What is 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.

Properties of AG 213

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 information for AG 213

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P304+P340:IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P405:Store locked up.