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AG-82 (Synonyms: NSC 676484,RG-50875,Tyrphostin 25,Tyrphostin AG-82)

Katalog-Nr.GC11845

AG-82 (AG82) ist ein spezifischer Inhibitor der EGFR-Tyrosinkinase.

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AG-82 Chemische Struktur

Cas No.: 118409-58-8

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AG-82 is a cell-permeable, reversible, and competitive inhibitor of tyrosine kinase and epidermal growth factor (EGF) receptor.

Protein tyrosine kinases (PTKs) have been involved in regulating cell proliferation, cell differentiation, and signaling processes in the immune system. Dysfunction of protein tyrosine kinases result in inflammatory responses and diseases including cancer, atherosclerosis, and psoriasis [2]. The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein. Activation of EGFR results in autophosphorylation of receptor tyrosine kinase and has been involved in regulating cellular proliferation, differentiation, and survival. Overexpression of EGFR has been identified in a variety of tumor cell lines and has been associated with poor prognosis and decreased survival [3].

In the human epidermoid carcinoma cell line A431, AG-82 inhibited the activity of epidermal growth factor receptor kinase with an IC50 value of 3 μM [1]. AG-82 inhibited the GTPase activity of transducin with an IC50 of 7 μM. AG-82 inhibited neuromedin B-induced phosphorylation of p125FAK (focal adhesion kinase). AG-82 blocked the induction of inducible nitric oxide synthase in glial cells and Induced apoptosis in human leukemic cell lines.

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] Levitzki A, Gazit A.  Tyrosine kinase inhibition: an approach to drug development[J]. Science, 1995, 267(5205): 1782.
[3] Herbst R S.  Review of epidermal growth factor receptor biology[J]. International Journal of Radiation Oncology Biology Physics, 2004, 59(2): S21-S26.

Chemical Properties

Cas No. 118409-58-8 SDF
Überlieferungen NSC 676484,RG-50875,Tyrphostin 25,Tyrphostin AG-82
Chemical Name 2-[(3,4,5-trihydroxyphenyl)methylene]-propanedinitrile
Canonical SMILES OC1=CC(/C=C(C#N)/C#N)=CC(O)=C1O
Formula C10H6N2O3 M.Wt 202.2
Löslichkeit ≤20mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.9456 mL 24.728 mL 49.456 mL
5 mM 0.9891 mL 4.9456 mL 9.8912 mL
10 mM 0.4946 mL 2.4728 mL 4.9456 mL
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