136831-48-6 Usage
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.
Check Digit Verification of cas no
The CAS Registry Mumber 136831-48-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,6,8,3 and 1 respectively; the second part has 2 digits, 4 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 136831-48:
(8*1)+(7*3)+(6*6)+(5*8)+(4*3)+(3*1)+(2*4)+(1*8)=136
136 % 10 = 6
So 136831-48-6 is a valid CAS Registry Number.
InChI:InChI=1/C16H14N2O2/c1-19-15-6-5-12(9-16(15)20-2)8-14(10-17)13-4-3-7-18-11-13/h3-9,11H,1-2H3/b14-8+
136831-48-6Relevant articles and documents
(Arene)Ru(II) complexes of epidermal growth factor receptor inhibiting tyrphostins with enhanced selectivity and cytotoxicity in cancer cells
Biersack,Zoldakova,Effenberger,Schobert
, p. 1972 - 1975 (2010)
Ru(η6-arene) complexes of epidermal growth factor receptor (EGFR) inhibiting tyrphostins 1a and 1b were prepared, characterized and tested for DNA interaction and bioactivity in four human tumor cell lines. The intrinsic cytotoxicity and cell line selectivity of o-hydroxyanisol 1a was greatly enhanced in its Ru(η6-p-cymene) complex 2a and in its Ru(η6-toluene) complex 3a. Complex 2a was particularly efficacious against multi-drug resistant EGFR(+) MCF-7/Topo breast carcinoma cells and also against mTOR-dependent EGFR(-) HL-60 leukemia cells. Complex 3a showed enhanced activity only against 518A2 melanoma cells and HL-60 cells, which are both known to express the mTOR protein. DNA was strongly metallated (ca. 1.7-2%) by all new Ru complexes without undergoing topological changes. Apparently, by complexation to Ru fragments tyrphostin derivatives can address additional biological targets in a manner instrumental to antitumoral strategies.
