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AG 99 (Synonyms: Tyrphostin 46, Tyrphostin AG-99)

Katalog-Nr.GC14494

AG 99 ((E)-Tyrphostin 46) ist ein potenter EGFR-Inhibitor.

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AG 99 Chemische Struktur

Cas No.: 122520-85-8

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AG 99 is a potent inhibitor of EGF receptor tyrosine kinase with IC50 value of 10 μM [1].

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation.

AG 99 is a potent and competitive EGFR tyrosine kinase inhibitor against both the substrate polyGAT and ATP [1]. In serum-starved human bladder carcinoma cell line 5637 cells, the 145-kDa protein, which was the β-subunit of c-Met/hepatocyte growth factor (HGF) receptor, was phosphorylated on 1003, 1234 and 1235 tyrosine residues. Also, tyrosine kinases EGFR and Src were activated. While, AG99 or inhibitors of Src (PP2, SU6656) significantly inhibited tyrosine phosphorylation of p145met and induced cell death through activation of caspase-like proteases. These results suggested that serum-independent growth of 5637 cells was involved by the tyrosine phosphorylation of p145met mediated by Src and EGFR [2].

References:
[1].  Gazit A, Osherov N, Gilon C, et al. Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro. J Med Chem, 1996, 39(25): 4905-4911.
[2].  Yamamoto N, Mammadova G, Song RX, et al. Tyrosine phosphorylation of p145met mediated by EGFR and Src is required for serum-independent survival of human bladder carcinoma cells. J Cell Sci, 2006, 119(Pt 22): 4623-4633.

Chemical Properties

Cas No. 122520-85-8 SDF
Überlieferungen Tyrphostin 46, Tyrphostin AG-99
Chemical Name (Z)-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide
Canonical SMILES OC1=CC(/C=C(C#N)\C(N)=O)=CC=C1O
Formula C10H8N2O3 M.Wt 204.18
Löslichkeit DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml 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 4.8976 mL 24.4882 mL 48.9764 mL
5 mM 0.9795 mL 4.8976 mL 9.7953 mL
10 mM 0.4898 mL 2.4488 mL 4.8976 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 31 reference(s) in Google Scholar.)

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