133550-41-1 Usage
Uses
AG 556 is a highly selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TK inhibitor). AG 556 has been shown to decrease human atrial IKur and cloned hKv1.5 channels by inhibiting EGFR TK.
Biological Activity
Epidermal growth factor receptor (EGFR) kinase inhibitor (IC 50 = 1.1 μ M). Selective over ErbB2 (IC 50 > 500 μ M).
references
[1]. zhang dy, zhang yh, sun hy, et al. epidermal growth factor receptor tyrosine kinase regulates the human inward rectifier potassium k(ir)2.3 channel, stably expressed in hek 293 cells. br j pharmacol, 2011 nov, 164(5): 1469-1478 [1].[2]. zhang dy, wu w, deng xl, et al. genistein and tyrphostin ag556 inhibit inwardly-rectifying kir2.1 channels expressed in hek 293 cells via protein tyrosine kinase inhibition. biochim biophys acta, 2011, 1808(8): 1993-1999.[3]. kleinberger-doron n, shelah n, capone r, et al. inhibition of cdk2 activation by selected tyrphostins causes cell cycle arrest at late g1 and s phase. exp cell res, 1998, 241(2): 340-351.[4]. sevransky je, shaked g, novogrodsky a, et al. tyrphostin ag 556 improves survival and reduces multiorgan failure in canine escherichia coli peritonitis. j clin invest, 1997, 99(8): 1966-1973.
Check Digit Verification of cas no
The CAS Registry Mumber 133550-41-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,3,5,5 and 0 respectively; the second part has 2 digits, 4 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 133550-41:
(8*1)+(7*3)+(6*3)+(5*5)+(4*5)+(3*0)+(2*4)+(1*1)=101
101 % 10 = 1
So 133550-41-1 is a valid CAS Registry Number.
InChI:InChI=1/C20H20N2O3/c21-14-17(12-16-9-10-18(23)19(24)13-16)20(25)22-11-5-4-8-15-6-2-1-3-7-15/h1-3,6-7,9-10,12-13,23-24H,4-5,8,11H2,(H,22,25)/b17-12+
133550-41-1Relevant articles and documents
Tyrphostins. 2. Heterocyclic and α-Substituted Benzylidenemalonitrile Tyrphostins as Potent Inhibitors of EGF Receptor and ErbB2/neu Tyrosine Kinases
Gazit, Aviv,Osherov, Nir,Posner, Israel,Yaish, Pnina,Poradosu, Enrique,et al.
, p. 1896 - 1907 (2007/10/02)
We have previously described a novel series of low molecular weight protein tyrosine kinase inhibitors which we named tyrphostins.The characteristic active pharmacophore of these compounds was the hydroxy-cis-benzylidenemalonitrile moiety.In this article we describe three novel groups of tyrphostins: (i) one group has the phenolic moiety of the cis-benzylidenemalononitrile replaced either with other substituted benzenes or with heteroaromatic rings, (ii) another is a series of conformationally constrained derivatives of hydroxy-cis-benzylidenemalononitriles in which the malononitrile moiety is fixed relative to the aromatic ring, and (iii) two groups of compounds in which the position trans to the benzenemalononitrile has been substituted by ketones and amides.Among the novel tyrphostins examined we found inhibitors which discriminate between the highly homologous EGF receptor kinase (HER1) and ErbB2/neu kinase (HER2).These findings may lead to selective tyrosine kinase blockers for the treatment of diseases in which ErbB2/neu is involved.