122520-90-5 Usage
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..
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.
Check Digit Verification of cas no
The CAS Registry Mumber 122520-90-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,2,5,2 and 0 respectively; the second part has 2 digits, 9 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 122520-90:
(8*1)+(7*2)+(6*2)+(5*5)+(4*2)+(3*0)+(2*9)+(1*0)=85
85 % 10 = 5
So 122520-90-5 is a valid CAS Registry Number.
InChI:InChI=1/C13H8N4O3/c14-4-8(12(17)9(5-15)6-16)1-7-2-10(18)13(20)11(19)3-7/h1-3,18-20H,17H2/b8-1+
122520-90-5Relevant articles and documents
Tyrphostins I: Synthesis and Biological Activity of Protein Tyrosine Kinase Inhibitors
Gazit, Aviv,Yaish, Pnina,Gilon, Chaim,Levitzki, Alexander
, p. 2344 - 2352 (2007/10/02)
A novel class of low molecular weight proteine kinase inhibitors is described.These compounds consitute a systematic series of molecules with a progressive increase in affinity toward the substrate site of the EGF receptor kinase domain.These competitive inhibitors also effectively block the EGF-dependent autophosphorylation of the receptor.The potent EGF receptor kinase blockers examined were found to competitively inhibit the homologous insulin receptor kinase at 102-103 higher inhibitor concentrations in spite of the significant homology between these protein tyrosine kinases.These results demonstrate the ability to synthesize selective tyrosine kinase inhibitors.The most potent EGF receptor kinase inhibitors also inhibit the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on EGF independent cell growth.These results demonstrate the potential use of protein tyrosine kinase inhibitors as selective antiproliferative agents for proliferative diseases caused by the hyperactivity of protein tyrosine kinases.We have suggested the name "tyrphostins" for this class of antiproliferative compounds which act as protein tyrosine kinase blockers.
