ホーム>>Signaling Pathways>> Microbiology & Virology>> Reverse Transcriptase>>AG 555

AG 555 (Synonyms: Tyrphostin AG-555, Tyrphostin B46)

カタログ番号GC11744

強力な抗レトロウイルス薬である AG 555 (Tyrphostin AG 555) は、EGFR の強力かつ選択的な阻害剤であり、Cdk2 の活性化をブロックします。

Products are for research use only. Not for human use. We do not sell to patients.

AG 555 化学構造

Cas No.: 133550-34-2

サイズ 価格 在庫数 個数
10mg
$79.00
Ship Within 7 Days
50mg
$315.00
Ship Within 7 Days

Tel:(909) 407-4943 Email: sales@glpbio.com

顧客レビュー

カスタマーレビューに基づきます。

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

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.
[2]. Baars S, et al. Tyrphostin AG 555 inhibits bovine papillomavirus transcription by changing the ratio between E2 transactivator/repressor function. J Biol Chem. 2003 Sep 26;278(39):37306-13.
[3]. Ben-Bassat H, et al. Tyrphostins that suppress the growth of human papilloma virus 16-immortalized human keratinocytes. J Pharmacol Exp Ther. 1999 Sep;290(3):1442-57.

Background

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.

Chemical Properties

Cas No. 133550-34-2 SDF
同義語 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
溶解度 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.
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

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
  • モルアリティ計算機

  • 希釈計算機

質量
=
濃度
x
容積
x
MW*
 
 
 
**ストックソリューションを準備する際には、常にバイアルラベルおよび MSDS/CoA(オンラインで利用可能)で掲載された製品のロット固有分子量を使用してください。

計算

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

レビュー

Review for AG 555

Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for AG 555

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.