AG 494 (Synonyms: Tyrphostin AG-494) |
| رقم الكتالوجGC17489 |
AG 494 (Tyrphostin AG 494) هو مثبط قوي وانتقائي لتيروزين كيناز EGFR (IC50 \u003d 0.7 ميكرومتر). يثبط AG 494 الفسفرة الذاتية لـ EGFR و ErbB2 و HER1-2 و PDGF-R مع IC50s 1.1 و 39 و 45 و 6 ميكرومتر ، على التوالي. يمنع AG 494 تنشيط Cdk2 ويمنع تخليق الحمض النووي المعتمد على عامل النمو البشري (EGF).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 133550-35-3
Sample solution is provided at 25 µL, 10mM.
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AG 494 is a potent and selective inhibitor of EGFR with IC50 value of 0.7 μM.
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 494 is a potent and selective EGFR inhibitor. AG 494 inhibited autophosphorylation of EGFR and HER-2 with IC50 values of 1.1 and 39 μM, respectively. In DHER-14 cells, AG 494 inhibited Cdk2 activation and EGF-dependent DNA synthesis [1]. AG494 arrested cells at late G1 and S phase and inhibited the activation of Cdk2 by phosphorylating tyrosine 15 on Cdk2 [2]. Epidermal growth factor (EGF) increased (bone morphogenetic protein) BMP9-induced osteogenic markers of mesenchymal stem cells (MSCs), which was inhibited by AG-494 in a time- and dose-dependent way [3]. In human prostate (DU145) and lung (A549) cancer cell lines, AG494 reversibly and significantly inhibited autocrine growth in a dose-dependent way. Also, AG494 induced cell apoptosis in both cell lines and arrested cell growth in the G1 phase [4].
References:
[1]. Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett, 1997, 410(2-3): 187-190.
[2]. 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.
[3]. Liu X, Qin J, Luo Q, et al. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med, 2013, 17(9): 1160-1172.
[4]. Bojko A1, Reichert K, Adamczyk A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol, 2012, 50(2): 186-195.
| Cas No. | 133550-35-3 | SDF | |
| المرادفات | Tyrphostin AG-494 | ||
| Chemical Name | (E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-phenylacrylamide | ||
| Canonical SMILES | OC1=CC(/C=C(C#N)/C(NC2=CC=CC=C2)=O)=CC=C1O | ||
| Formula | C16H12N2O3 | M.Wt | 280.28 |
| الذوبان | DMF: 30 mg/ml,DMF:PBS (pH7.2) (1:1): 0.5 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml | Storage | 4°C, protect from light |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5679 mL | 17.8393 mL | 35.6786 mL |
| 5 mM | 0.7136 mL | 3.5679 mL | 7.1357 mL |
| 10 mM | 0.3568 mL | 1.7839 mL | 3.5679 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
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Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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