Home >> AG-183
Related Products
AG-183
inhibitor of epidermal growth factor (EGF) receptor kinase

Catalog No.C4844
Size Price Stock Qty
10mg
$73.00
In stock
25mg
$173.00
In stock
50mg
$307.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

AG-183

AG-183 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

AG-183 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 122520-90-5 SDF Download SDF
Synonyms Tyrphostin 51
Chemical Name 2-amino-4-(3,4,5-trihydroxyphenyl)-1,3-butadiene-1,1,3-tricarbonitrile
Canonical SMILES OC1=C(O)C(O)=CC(/C=C(C#N)/C(N)=C(C#N)\C#N)=C1
Formula C13H8N4O3 M.Wt 268.2
Solubility ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

AG-183, a member of tyrphostin, is an inhibitor of protein tyrosine kinase [1].

Protein tyrosine kinase is an enzyme that catalyzes the transfer of the γ phosphate of ATP to tyrosine residues on protein substrates. Phosphorylation of proteins by kinases is an important mechanism in signal transduction and regulating cellular activity, such as cell division. Tyrosine phosphorylation is a key covalent modification that occurs in multicellular organisms as a result of intercellular communication during embryogenesis and maintenance of adult tissues. Phosphorylation of tyrosine residues modulates enzymatic activity and creates binding sites for the recruitment of downstream signaling proteins [2].

PTK inhibitors could preferentially inhibit the epidermal growth factor (EGF) receptor kinase to block EGF-dependent cell proliferation [1]. In the human epidermoid carcinoma cell line, A431AG-183 inhibited the activity of epidermal growth factor (EGF) receptor kinase with an IC50 value of 800 nM [1].

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.