122520-90-5 Usage
Description
TYRPHOSTIN A51, a member of the Tyrphostin family, is a protein tyrosine kinase (PTK) inhibitor specifically targeting the epidermal growth factor (EGF) receptor kinase. It functions as a potent antiproliferative agent, exhibiting mixed competitive inhibition with ATP and substrate, and is instrumental in managing diseases driven by the hyperactivity of PTKs.
Uses
Used in Pharmaceutical Industry:
TYRPHOSTIN A51 is used as an antiproliferative agent for treating diseases caused by the hyperactivity of protein tyrosine kinases. Its ability to inhibit EGFRK activity makes it a promising candidate for managing conditions associated with uncontrolled cell proliferation.
Used in Cancer Research:
In cancer research, TYRPHOSTIN A51 is utilized as a potent inhibitor of EGFRK activity, playing a crucial role in studying the mechanisms of EGF-dependent cell proliferation and the development of targeted therapies for cancer treatment.
Used in Drug Development:
TYRPHOSTIN A51 serves as a key component in the development of novel drugs that target the epidermal growth factor receptor kinase, potentially leading to the creation of more effective treatments for various cancers and other diseases related to PTK hyperactivity.
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.
