140674-76-6 Usage
Description
Tyrphostins are tyrosine phosphorylation inhibitors that act by inhibiting tyrosine kinases. AG957 is a tyrphostin that targets transforming Bcr-Abl fusion proteins (p185Bcr-Abl, p210Bcr-Abl), as well as normal c-Abl (IC50s = 4.3, 1, and 7.1 μM, respectively, for human proteins). It also inhibits epidermal growth factor receptor (IC50 = 0.25 μM). As the constitutively-active 210 kDa Bcr-Abl fusion protein commonly occurs in chronic myelogenous leukemia (CML) cells, AG957 is commonly used to study Bcr-Abl signaling in the CML K562 cell line. AG957 is also used to study signaling through c-Abl.
Uses
Tyrphostin AG 957 is a potent tyrosine kinase inhibitor. Also, it causes metabolic alterations in K562 cells. It is a COVID19-related research product.
references
[1]. anafi m, gazit a, gilon c, et al. selective interactions of transforming and normal abl proteins with atp, tyrosine-copolymer substrates, and tyrphostins. j biol chem. 1992 mar 5;267(7):4518-23.[2]. kaur g, gazit a, levitzki a, et al. tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in k562 chronic myelogenous leukemia. anticancer drugs. 1994 apr;5(2):213-22.[3]. jamieson l, carpenter l, biden tj, et al. protein kinase ciota activity is necessary for bcr-abl-mediated resistance to drug-induced apoptosis. j biol chem. 1999 feb 12;274(7):3927-30.[4]. fu p, usatyuk pv, lele a, et al. c-abl mediated tyrosine phosphorylation of paxillin regulates lps-induced endothelial dysfunction and lung injury. am j physiol lung cell mol physiol. 2015 may 15;308(10):l1025-38.
Check Digit Verification of cas no
The CAS Registry Mumber 140674-76-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,0,6,7 and 4 respectively; the second part has 2 digits, 7 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 140674-76:
(8*1)+(7*4)+(6*0)+(5*6)+(4*7)+(3*4)+(2*7)+(1*6)=126
126 % 10 = 6
So 140674-76-6 is a valid CAS Registry Number.
140674-76-6Relevant articles and documents
Synthesis and biological evaluation of platensic alcohol as an adamantane surrogate in antitumor drug lead adaphostin
Duan, Yanwen,Huang, Yong,Wen, Zhongqing,Xiong, Yi
, (2021/07/28)
Adamantane has been widely used as a “lipophilic bullet” in drug discovery and development, due to its unique diamond-like architecture with benign pharmacological/ pharmaceutical properties. Platensimycin is a natural product isolated from a soil streptomycete, which contains an adamantane-like moiety extensively modified from a diterpenoid precursor. In the current study, platensic alcohol was semisynthesized from platensimycin and used as an adamantane surrogate in anticancer drug lead adaphostin. The resulting hybrid platensic alcohol/adaphostin compounds, eg. 4a and 4b, exhibited similar cytotoxic activity with adaphostin against the tested cancer cell lines. In particular, 4b generates significantly more reactive oxygen species (ROS) and shows stronger synergy with the clinically used histone deacetylase inhibitor vorinostat than adaphostin, probably due to the presence of two hydroquinone groups. Density functional theory calculation supports that there could be certain π-π stacking interaction in 4b in aqueous solution, which might explain that 4b has similar serum stability with adaphostin. Our study not only leads to the identification of 4b as a potent ROS generating agent, but showcases a simple scaffold hopping strategy to harvest lipophilic scaffolds from natural products.
COMPOUNDS FOR THE TREATMENT OF DISORDERS RELATED TO VASCULOGENESIS AND/OR ANGIOGENESIS
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, (2008/06/13)
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Compounds for the treatment of disorders related to vasculogenesis and/or angiogenesis
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, (2008/06/13)
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is bas
