TYRPHOSTIN RG 13022
Synonym(s):2-(3,4′-Dimethoxyphenyl)-1-(3″-pyridinyl)acrylonitrile
- CAS NO.:136831-48-6
- Empirical Formula: C16H14N2O2
- Molecular Weight: 266.29
- MDL number: MFCD00236444
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-05 08:26:49
What is TYRPHOSTIN RG 13022?
The Uses of TYRPHOSTIN RG 13022
RG-13022 is an epidermal growth factor (EGF) inhibitor and PDGF receptor tyrosine kinases.
What are the applications of Application
RG-13022 is an inhibitor of the EGF 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].
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.
Properties of TYRPHOSTIN RG 13022
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 for TYRPHOSTIN RG 13022
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. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for TYRPHOSTIN RG 13022
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