AG 99

EGFR inhibitor CAS# 122520-85-8

AG 99

Catalog No. BCC6667----Order now to get a substantial discount!

Product Name & Size Price Stock
AG 99:10mg $136.00 In stock
AG 99:20mg $231.00 In stock
AG 99:50mg $544.00 In stock
AG 99:100mg $952.00 In stock
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Quality Control of AG 99

Number of papers citing our products

Chemical structure

AG 99

3D structure

Chemical Properties of AG 99

Cas No. 122520-85-8 SDF Download SDF
PubChem ID 5328768 Appearance Powder
Formula C10H8N2O3 M.Wt 204.18
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 165 mg/mL (808.11 mM; Need ultrasonic)
Chemical Name (E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
SMILES C1=CC(=C(C=C1C=C(C#N)C(=O)N)O)O
Standard InChIKey USOXQZNJFMKTKJ-XVNBXDOJSA-N
Standard InChI InChI=1S/C10H8N2O3/c11-5-7(10(12)15)3-6-1-2-8(13)9(14)4-6/h1-4,13-14H,(H2,12,15)/b7-3+
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of AG 99

DescriptionEpidermal growth factor receptor (EGFR) kinase inhibitor (IC50 = 10 μM) that is selective over insulin receptor kinase. Blocks tyrosine phosphorylation of p145met and promotes cell death of normal and cancer cells via activation of caspase-like proteases in vitro.

AG 99 Dilution Calculator

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AG 99 Molarity Calculator

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Preparing Stock Solutions of AG 99

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.8976 mL 24.4882 mL 48.9764 mL 97.9528 mL 122.441 mL
5 mM 0.9795 mL 4.8976 mL 9.7953 mL 19.5906 mL 24.4882 mL
10 mM 0.4898 mL 2.4488 mL 4.8976 mL 9.7953 mL 12.2441 mL
50 mM 0.098 mL 0.4898 mL 0.9795 mL 1.9591 mL 2.4488 mL
100 mM 0.049 mL 0.2449 mL 0.4898 mL 0.9795 mL 1.2244 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on AG 99

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.

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References on AG 99

Li/Ag ratio dependent structure and upconversion photoluminescence of Li(x)Ag(1-x)Yb(0.99)(MoO4)(2):0.01Er(3+) phosphors.[Pubmed:25557109]

Phys Chem Chem Phys. 2015 Feb 7;17(5):3689-96.

A series of double molybdate scheelite-type phosphors LixAg1-xYb0.99(MoO4)2:0.01Er(3+) (x = 0, 0.1, 0.3, 0.5, 0.7, 0.9, 1.0) were synthesized by the solid state reaction method, and their crystal structures and upconversion (UC) luminescence properties were investigated in detail. The phase structure evolution of this series samples was discussed and the selected Li0.5Ag0.5Yb0.99(MoO4)2:0.01Er(3+) was analyzed based on the Rietveld refinement. The UC emission properties and the related UC mechanism were also studied. With an increasing Li/Ag ratio in this host, the UC emission intensities of LixAg1-xYb0.99(MoO4)2:0.01Er(3+) increased obviously, and the enhancement could be attributed to the coupling effect and the nonradiative transition between two energy levels of LixAg1-xYb(MoO4)2 matrices and the activator Er(3+), which have also been analyzed based on the results of the ultraviolet-visible diffuse reflection spectroscopy (UV-vis DRS) and Raman spectroscopy.

AG 60.99: A promising contrast agent for computed tomography of the liver and spleen.[Pubmed:185647]

Radiology. 1976 Nov;121(2):491.

AG 60.99, an emulsion of poppy-seed oil, is proposed as a promising organ-specific agent for computed tomography (CT) of the liver and spleen. This agent not only opacifies the hepatic parenchyma enough to enhance visualization of the bile ducts but also demonstrates the vascular anatomy with smaller doses than those required for conventional studies.

Tyrosine phosphorylation of p145met mediated by EGFR and Src is required for serum-independent survival of human bladder carcinoma cells.[Pubmed:17062641]

J Cell Sci. 2006 Nov 15;119(Pt 22):4623-33.

Here we address the molecular mechanism of serum-independent survival and growth of human bladder carcinoma cell line 5637. Serum starvation promoted tyrosine phosphorylation of a 145-kDa protein and activation of the tyrosine kinase Src and the receptor for epidermal growth factor (EGFR) over a slow time course (>8 hours). The phosphorylated 145-kDa protein was identified as the beta-subunit of c-Met/hepatocyte growth factor (HGF) receptor, p145(met), in which tyrosine residues 1003, 1234, and 1235 were phosphorylated. Inhibitors of Src (PP2, SU6656) or EGFR (AG99), but not p145(met) (K252a), effectively blocked tyrosine phosphorylation of p145(met) and promoted cell death accompanied by activation of caspase-like proteases. Conditioned medium from the serum-starved 5637 cells or purified EGF readily promoted the activation of Src and EGFR, and tyrosine phosphorylation of p145(met) in normally grown 5637 cells, suggesting that autocrine signaling of EGFR ligands is responsible for signal transduction events in serum-starved cells. Consistent with this idea, a monoclonal antibody against EGFR that would interfere with the ligand binding to EGFR blocked tyrosine phosphorylation events and promoted the caspase activation and cell death in serum-free conditions. Such apoptotic cell death was also induced by pretreatment of cells with a high concentration of HGF that downregulated endogenous p145(met). Nevertheless, Cu2+ ions, competitive inhibitors for HGF-binding to p145(met), did not show any effect on cellular functions in serum-free conditions. These results suggest that the serum-independent growth of 5637 cells involves the transmembrane signaling cascade via EGFR ligand(s) (but not HGF), EGFR, Src and p145(met).

Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro.[Pubmed:8960549]

J Med Chem. 1996 Dec 6;39(25):4905-11.

Benzylidenemalononitrile (BMN) tyrphostins were previously found to be potent inhibitors of EGF receptor (EGFR) tyrosine kinase activity. Since these compounds were found to compete for the substrate and sometimes with the ATP site and since EGFR acts as a dimer, we prepared a series of dimeric tyrphostins. These dimeric tyrphostins were built from two BMN units linked by various spacers and designed to fit the dimeric cross-autophosphorylation signal transduction intermediate of the EGFR tyrosine kinases. Structure-activity relationship of these potent dimeric EGF receptor tyrosine kinase inhibitors is reported.

Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.[Pubmed:2552117]

J Med Chem. 1989 Oct;32(10):2344-52.

A novel class of low molecular weight protein tyrosine kinase inhibitors is described. These compounds constitute a systematic series of molecules with a progressive increase in affinity toward the substrate site of the EGF receptor kinase domain. These competitive inhibitors also effectively block the EGF-dependent autophosphorylation of the receptor. The potent EGF receptor kinase blockers examined were found to competitively inhibit the homologous insulin receptor kinase at 10(2)-10(3) higher inhibitor concentrations in spite of the significant homology between these protein tyrosine kinases. These results demonstrate the ability to synthesize selective tyrosine kinase inhibitors. The most potent EGF receptor kinase inhibitors also inhibit the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on EGF independent cell growth. These results demonstrate the potential use of protein tyrosine kinase inhibitors as selective antiproliferative agents for proliferative diseases caused by the hyperactivity of protein tyrosine kinases. We have suggested the name "tyrphostins" for this class of antiproliferative compounds which act as protein tyrosine kinase blockers.

Description

(E)-AG 99 ((E)-Tyrphostin 46; (E)-Tyrphostin AG 99) is a potent EGFR inhibitor.

Keywords:

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