AG 555 (Synonyms: Tyrphostin AG-555, Tyrphostin B46) |
| رقم الكتالوجGC11744 |
AG 555 (Tyrphostin AG 555) ، دواء فعال مضاد للفيروسات القهقرية ، هو مثبط قوي وانتقائي لـ EGFR ويمنع تنشيط Cdk2
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Cas No.: 133550-34-2
Sample solution is provided at 25 µL, 10mM.
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AG 555 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 555 is a potent and selective EGFR inhibitor. In HPV16-immortalized human keratinocytes, AG 555 inhibited the activation of Cdk2 and induced growth arrest at the G1 phase accompanied by 15-20% cell apoptosis [1]. AG556 arrested cells at G1/S phase by 85% and inhibited the activation of Cdk2 by phosphorylating tyrosine 15 on Cdk2 [2]. In A-498, Caki-1 and Caki-2 renal carcinoma cell lines and RT4, J82 and T24 transitional carcinoma cell lines, AG555 inhibited cell proliferation with IC50 values ranging from 3 to 16 μM in a dose-dependent way. AG555 (10-30 μM) completely inhibited cell growth [3]. In NIH/3T3 cells infected with Moloney murine leukemia virus (Mo-MuLV), AG-555 inhibited the viral DNA integrated into the host genome in acutely infected cells. While in chronically infected cells, AG-555 decreased the level of viral RNA and inhibited viral protein synthesis [4].
References:
[1]. Ben-Bassat H, Rosenbaum-Mitrani S, Hartzstark Z, et al. Inhibitors of epidermal growth factor receptor kinase and of cyclin-dependent kinase 2 activation induce growth arrest, differentiation, and apoptosis of human papilloma virus 16-immortalized human keratinocytes. Cancer Res, 1997, 57(17): 3741-3750.
[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]. Sion-Vardy N, Vardy D, Rodeck U, et al. Antiproliferative effects of tyrosine kinase inhibitors (tyrphostins) on human bladder and renal carcinoma cells. J Surg Res, 1995, 59(6): 675-680.
[4]. Seri I, Aflalo E, Gazit A, et al. Tyrphostin AG-555 inhibits early and late stages of Moloney murine leukemia virus replication cycle. Int J Oncol, 1997, 10(6): 1185-1189.
Cell experiment: | ID13 mouse fibroblasts are maintained in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 100 units/mL Penicillin, and 100 μg/mL Streptomycin. Cells are seeded at 2.5×104 cells/cm2 to ensure logarithmic growth. The final concentration of the Tyrphostin AG 555 is 30 μM in all experiments. Stock solutions of 10 mM in Me2SO are stored at -80°C. To exclude potential Me2SO effects, the same final concentrations (0.3%) of Me2SO are added to nontreated controls. Actinomycin D is dissolved in water and added to cells in a final concentration of 5 μg/mL. SB 203580 is dissolved in Me2SO (stock concentration: 50 mM) and used in a final concentration of 10 μM[2]. |
References: [1]. Michaelis M, et al. Cisplatin-resistant neuroblastoma cells express enhanced levels of epidermal growth factor receptor (EGFR) and are sensitive to treatment with EGFR-specific toxins. Clin Cancer Res. 2008 Oct 15;14(20):6531-7. | |
| Cas No. | 133550-34-2 | SDF | |
| المرادفات | Tyrphostin AG-555, Tyrphostin B46 | ||
| Chemical Name | (E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-(3-phenylpropyl)acrylamide | ||
| Canonical SMILES | O=C(/C(C#N)=C/C(C=C1O)=CC=C1O)NCCCC2=CC=CC=C2 | ||
| Formula | C19H18N2O3 | M.Wt | 322.36 |
| الذوبان | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 20 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. |
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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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1021 mL | 15.5106 mL | 31.0212 mL |
| 5 mM | 0.6204 mL | 3.1021 mL | 6.2042 mL |
| 10 mM | 0.3102 mL | 1.5511 mL | 3.1021 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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