TYRPHOSTIN A51 Chemical Properties

Melting point:

275 °C

Boiling point:

788.2±60.0 °C(Predicted)

Density 

1.591±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

≤20mg/ml in DMSO;20mg/ml in dimethyl formamide

form 

Orange solid.

pka

8.46±0.15(Predicted)

Safety Information

WGK Germany 

3

HazardClass 

6.1

MSDS

• Language:English Provider:SigmaAldrich

TYRPHOSTIN A51 Usage And Synthesis

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 which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. AG-183 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC₅₀ value of 0.8 μM in the human epidermoid carcinoma cell line A431.

Uses

Tyrphostin 51 is a potent inhibitor of EGFRK activity showing mixed competitive inhibition with ATP and substrate1-3..

Definition

ChEBI: 2-amino-4-(3,4,5-trihydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile is a benzenetriol.

References

[1] 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.
[2] hubbard s r, till j h. protein tyrosine kinase structure and function[j]. annual review of biochemistry, 2000, 69(1): 373-398.

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