TYRPHOSTIN RG 13022 Chemical Properties

Melting point:

116.0 to 120.0 °C

Boiling point:

423.8±45.0 °C(Predicted)

Density 

1.172±0.06 g/cm3(Predicted)

storage temp. 

Keep in dark place,Sealed in dry,2-8°C

solubility 

DMSO or ethanol: soluble

form 

White solid.

pka

3.03±0.12(Predicted)

color 

White to Yellow to Green

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

HS Code 

2933.39.9200

MSDS

• Language:English Provider:SigmaAldrich

TYRPHOSTIN RG 13022 Usage And Synthesis

Uses

RG-13022 is an epidermal growth factor (EGF) inhibitor and PDGF receptor tyrosine kinases.

Biological Activity

rg13022 is a egfr tyrosine kinase inhibitor.increased expression of various growth factor receptors including egfr has been observed in human tumours. one therapeutic strategy for overcoming egf autocrine control of tumour growth is to inhibit egfr protein tyrosine kinase.

in vitro

rg13022 had a dose-dependent, antiproliferative effect on gastric cell lines when grown either in serum-free conditions or in the presence of fcs. western blotting showed that rg13022 treatment led to an inhibition of the egfr phosphorylation in a431 cells and both egfr and c-erbb-2 in mkn45 cells. furthermore, investigation of intracellular signalling pathways suggested that alterations in intracellular signalling were responsible for the actions of rg 13022 in these cells [1].

in vivo

in rats, rg13022 showed rapid bi-exponential elimination from plasma with a terminal half-life of 50.4 min. rg13022 plasma concentrations were less than 1 μm by 20 min after injection. in addition, rg13022 had no influence on the growth of hn5 tumours when administered chronically, starting either on the tumour inoculation day or after establishment of tumour xenografts. the rapid in-vivo elimination of rg13022 had potential significance to its development, as plasma concentrations fell below that required for in-vitro activity by 20 min after injection [2].

IC 50

5 μm for egfr

References

[1] mclaughlin m,brunton v,morrison v,rae a,cooke t,bartlett j. growth inhibition of gastric cancer cell lines by the tyrphostin rg13022 and its effects on intracellular signalling. int j oncol.1996 mar;8(3):589-96.
[2] mcleod hl,brunton vg,eckardt n,lear mj,robins dj,workman p,graham ma. in vivo pharmacology and anti-tumour evaluation of the tyrphostin tyrosine kinase inhibitor rg13022. br j cancer.1996 dec;74(11):1714-8.

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